Синтез N-ацилсульфонамідів: від загальновідомих реакцій ацилювання до сучасних каталітичних і сталих методів
N-Acyl sulfonamides are widely used bioisosteres of carboxylic acids, valued for their favorable physicochemical and pharmacokinetic properties as well as their frequent occurrence in drug-like molecules. This review summarizes the principal synthetic approaches to these motifs, covering both establ...
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V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine
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Ukrainica Bioorganica Acta| _version_ | 1869381602726903808 |
|---|---|
| author | Gavrylenko, Oleksii V. Sosunovych, Bohdan S. Vashchenko, Bohdan V. Grygorenko, Oleksandr O. Moroz, Yurii S. |
| author_facet | Gavrylenko, Oleksii V. Sosunovych, Bohdan S. Vashchenko, Bohdan V. Grygorenko, Oleksandr O. Moroz, Yurii S. |
| author_institution_txt_mv | [
{
"author": "Oleksii V. Gavrylenko",
"institution": "Enamine Ltd., Kyiv, Ukraine"
},
{
"author": "Bohdan S. Sosunovych",
"institution": "Enamine Ltd., Kyiv, Ukraine"
},
{
"author": "Bohdan V. Vashchenko",
"institution": "Taras Shevchenko National University of Kyiv, Kyiv, Ukraine; Enamine Scientific Research Institute (SRI), Kyiv, Ukraine"
},
{
"author": "Oleksandr O. Grygorenko",
"institution": "Enamine Ltd., Kyiv, Ukraine; Taras Shevchenko National University of Kyiv, Kyiv, Ukraine; Enamine Scientific Research Institute (SRI), Kyiv, Ukraine"
},
{
"author": "Yurii S. Moroz",
"institution": "Enamine Ltd., Kyiv, Ukraine; Enamine Scientific Research Institute (SRI), Kyiv, Ukraine; Chemspace LLC, Kyiv, Ukraine"
}
] |
| author_sort | Gavrylenko, Oleksii V. |
| baseUrl_str | https://bioorganica.com.ua/index.php/journal/oai |
| collection | OJS |
| datestamp_date | 2026-06-29T15:59:56Z |
| description | N-Acyl sulfonamides are widely used bioisosteres of carboxylic acids, valued for their favorable physicochemical and pharmacokinetic properties as well as their frequent occurrence in drug-like molecules. This review summarizes the principal synthetic approaches to these motifs, covering both established and emerging methodologies, with emphasis on catalytic, green, and operationally simple approaches. Common strategies include direct N-acylation of sulfonamides and N-sulfonylation of carboxamides, as well as transformations employing sulfonyl azides, sulfonyl isocyanates, and related multicomponent processes. Recent developments, such as recyclable heterogeneous catalysts, solvent-free and aqueous conditions, carbonylative and photocatalytic S-N couplings, and mild transition-metal-mediated reactions highlight simplicity and sustainability. Collectively these advances provide an adaptable and efficient synthetic toolbox for accessing diverse N-acyl sulfonamides relevant to modern organic and medicinal chemistry. |
| doi_str_mv | 10.15407/bioorganica2025.02.013 |
| first_indexed | 2026-02-08T07:59:48Z |
| format | Article |
| fulltext |
ISSN 1814-9758. Ukr. Bioorg. Acta, 2025, Vol. 20, N 2
UDC 547.551.525.211.1
DOI: https://doi.org/10.15407/bioorganica2025.02.013
13
REVIEW ARTICLE
Synthesis of N-acyl sulfonamides: from common acylation reactions
to modern catalytic and sustainable methods
Oleksii V. Gavrylenko1, Bohdan S. Sosunovych1, Bohdan V. Vashchenko2,3*,
Oleksandr O. Grygorenko1,2,3, Yurii S. Moroz1,2,4
1 Enamine Ltd. (www.enamine.net), Kyiv, Ukraine
2 Taras Shevchenko National University of Kyiv, Kyiv, Ukraine
3 Enamine Scientific Research Institute (ESRI), Kyiv, Ukraine
4 Chemspace LLC, Kyiv, Ukraine
Abstract: N-Acyl sulfonamides are widely used bioisosteres of carboxylic acids, valued for their favorable physicochemical and
pharmacokinetic properties as well as their frequent occurrence in drug-like molecules. This review summarizes the principal synthetic
approaches to these motifs, covering both established and emerging methodologies, with emphasis on catalytic, green, and operationally
simple approaches. Common strategies include direct N-acylation of sulfonamides and N-sulfonylation of carboxamides, as well as
transformations employing sulfonyl azides, sulfonyl isocyanates, and related multicomponent processes. Recent developments, such as
recyclable heterogeneous catalysts, solvent-free and aqueous conditions, carbonylative and photocatalytic S-N couplings, and mild
transition-metal-mediated reactions highlight simplicity and sustainability. Collectively these advances provide an adaptable and efficient
synthetic toolbox for accessing diverse N-acyl sulfonamides relevant to modern organic and medicinal chemistry.
Keywords: N-acyl sulfonamides; green chemistry; catalysis; bioisosteres.
Introduction
N-Acyl sulfonamides are widely recognized in medicinal
chemistry as valuable bioisosteres of carboxylic acids, and
occupy a great range of acidic compounds in chemical
libraries [1-3]. Their structural features allows for precise
tuning of metabolic stability and binding affinity [1, 4]
which in turn has driven the discovery and development of
numerous medicinals, i.e., parecoxib [5-8] sulfacetamide [8-
10] acetyl sulfisoxazole [8, 11-13] etc. (see Figure 1).
According to the literature data, the most common
strategies for the synthesis of N-acyl sulfonamides can be
summarized as shown in Figure 2, where the key sulfonyl
fragment is used as a common precursor in reactions with
various electrophilic or nucleophilic partners.
Received:
Revised:
Accepted:
Published online:
10.09.2025
23.09.2025
20.10.2025
31.12.2025
Corresponding author. Tel.: +380-93-924-5594;
e-mail: vashchenko@knu.ua (B.V. Vashchenko)
ORCID: 0000-0003-4575-2065
S
Parecoxib
N
O
N
H
O
O
O
H2N
S
HN
O
O
O
Sulfacetamide
H2N
S
N
O
O
O
Acetyl sulfisoxazole
O N
Figure 1. N-Acyl sulfonamide medicinals.
In particular, various electrophilic or nucleophilic
partners. In particular, the reported methods rely on the use
of sulfonamides, sulfonyl azides, sulfonyl isocyanates,
sodium sulfonate salts, triazole derivatives, or alternatively,
include the sulfonylation of amides. The following sections
discuss each of these strategies in detail.
© Gavrylenko O.V. et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits
unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
Ukrainica Bioorganica Acta
www.bi oorgan ica . com.u a
mailto:vashchenko@knu.
https://orcid.org/0000-0003-4575-2065
ISSN 1814-9758. Ukr. Bioorg. Acta, 2025, Vol. 20, N 2
14
Figure 2. Main synthetic approaches to the synthesis of N-acyl
sulfonamides.
Acylation of sulfonamides
A simple and efficient approach involves the direct
acylation of sulfonamides using symmetrical anhydrides in
the presence of a catalytic amount of H2SO4 (Scheme 1).
The reaction is carried out in MeCN at 60 °C and
demonstrates high efficiency, with the yields were up to
98%. Overall, neither steric nor electronic effects of the
sulfonamide moiety significantly influenced the yield [14].
N
H
S
R1
O
O
R2
O
NH2
S
R1
O
O
N
H
S
t-Bu
O
O
Me
O
N
H
S
Me
O
O
Ph
O
N
H
S
Ph
O
O
CF3
O
(R2CO)2O
N
H
S
Ph
O
O
t-Bu
O
60% 44% 86%
94%
N
H
S
Me
O
O
t-Bu
O
94%
N
H
S
t-Bu
O
O
t-Bu
O
61%
H2SO4 (cat.)
MeCN, 60 °C
16 examples,
up to 98% yields
R1, R2 = Ar, Alk
Scheme 1. Synthesis of acyl sulfonamides by acylation with
symmetrical anhydrides (selected examples are given).
Another simple and efficient approach involves the
acylation of N-fluorophenyl sulfonamides with acyl
chlorides in pyridine, which serves both as a solvent and as
a base (Scheme 2). These compounds proved to be effective
N-acylating agents, providing good chemoselectivity and
high yields (up to 92%) when reacting with various
aromatic and aliphatic substrates [15].
Another promising strategy for the synthesis of N-acyl
sulfonamides involves the acylation reactions catalyzed by
silica phosphoric acid (Schemes 3-4). This approach is
applicable to both symmetrical carboxylic anhydrides and
acyl chlorides; moreover, the reaction is characterized by
operational simplicity and environmental friendliness due to
the mild conditions and the use of solvent-free approach or
heterogeneous systems at 80 °C. The method provides good
to excellent yields (up to 98%), and the isolated products
exhibit high purity after minimal work-up. Importantly,
silico-phosphoric acid can be reused at least three times
without a noticeable loss of catalytic activity [16].
N
S
R1
O
O
R3
O
NH
S
R1 O
O
N
S
Me
O
O
OBn
O
N
S
Me
O
O
OBn
O
N
S
Tol
O
O
OBn
O
R3COCl
N
S
Me
O
O
OBn
O
70%
90% 74% 39%
pyridine, rt
>15 examples,
up to 92% yields
R1 = Ar, Alk; R2 = Ar;
R3 = Cbz, Ph, t-BuR2
R2
F
F
CF3F
N
S
Me
O
O
Ph
O
92%
F
N
S
Me
O
O
t-Bu
O
84%
F
Scheme 2. Synthesis of acylated sulfonamides from carboxylic
acid chlorides (selected examples are given).
N
H
S
R1
O
O
R2
O
NH2
S
R1 O
O
N
H
S
Tol
O
O
Me
O
N
H
S
Ph
O
O
i-Pr
O
N
H
S
Ph
O
O
Me
O
N
H
S
Tol
O
O
Et
O
n-hexane, 85%;
neat, 80%
n-hexane, 97%;
neat, 95%
n-hexane, 87%;
neat, 95%
n-hexane 83%;
neat, 80%
n-hexane, reflux, or
neat 80 °C
15 examples,
up to 98% yields
R1 = Ar, Alk;
R2 = Alk
N
H
S
Me
O
O
Et
O
n-hexane, 87%;
neat, 82%
N
H
S
Me
O
O
i-Pr
O
n-hexane, 98%;
neat, 96%
(R2CO)2O, silico-
phosphoric acid (cat.)
Scheme 3. Acylation of sulfonamides with carboxylic anhydrides
in the presence of silico-phosphoric acid as a catalyst (selected
examples are given).
Lewis acids serve as other efficient catalysts for the
acylation of sulfonamides with carboxylic anhydrides
(Scheme 5). Studies have shown that BF3·Et2O, ZnCl2,
MoCl5, TiCl4, B(C6F5)3, Sc(OTf)3, and even I2, can catalyze
the reaction to form the desired products. Among the tested
catalysts, ZnCl2 demonstrated the optimal balance in the
activity, allowing for the efficient use of less reactive
anhydrides, e.g., benzoic or pivalic anhydride. Furthermore,
it was found that carboxylic acids themselves can also act as
acylating agents in the presence of ZnCl2 (Scheme 6) [17].
The arsenal of methods also contains the direct and mild
N-acylation of sulfonamides using esters as acylating agents
(Scheme 7). Several Lewis acids were studied as promoters,
among which TiCl4 proved to be the most effective,
O.V. Gavrylenko et al.
15
affording high yields of the target N-acyl sulfonamides (up
to 97%). As in the previous examples, the simplicity of both
the reaction procedure and product isolation could be
highlighted [18].
N
H
S
Tol
O
O
Ph
O
N
H
S
Ph
O
O
Me
O
N
H
S
Ph
O
O
Ph
O
N
H
S
Tol
O
O
Me
O
n-hexane, 90%;
neat, 82%
n-hexane, 82%;
neat, 80%
n-hexane, 82%;
neat, 80%
n-hexane, 87%;
neat, 75%
15 examples,
up to 90% yields
R1 = Ar, Alk;
R2 = Ar
N
H
S
Me
O
O
Ph
O
n-hexane, 89%;
neat, 80%
N
H
S
Me
O
O
Me
O
n-hexane, 80%;
neat, 85%
N
H
S
R1
O
O
R2
O
NH2
S
R1 O
O
n-hexane, reflux, or
neat, 80 °C
R2COCl, silico-
phosphoric acid (cat.)
Scheme 4. Acylation of sulfonamides with carboxylic acid
chlorides in the presence of silico-phosphoric acid (selected
examples are given).
N
S
R2
R1
O
O
R3
O
NH
S
R2
R1
O
O
N
H
S
Ph
O
O
Ph
O
N
H
S
Ph
O
O
CF3
O
N
H
S
Ph
O
O
Me
O
(R3CO)2O
N
H
S
Tol
O
O
Me
O
97% 94% 88%
97%
N
H
S
Me
O
O
Me
O
98%
N
Bn
S
Me
O
O
Me
O
95%
ZnCl2 (cat.)
CH2Cl2, rt
17 examples,
up to 98% yields
R1 = Ar, Alk; R2 = H, Alk;
R3= Me, Et, nPr, tBu, Ph
Scheme 5. N-Acylation of sulfonamides with carboxylic
anhydrides in the presence of ZnCl2 as a catalyst (selected
examples are given).
N
H
S
R1
O
O
R2
O
NH2
S
R1
O
O
N
H
S
Ph
O
O O
N
H
S
Tol
O
O O
N
H
S
Ph
O
O O
R2CO2H
N
H
S
Ph
O
O O
80% 84%
82%
80%
85%
N
H
S
Me
O
O O
82%
ZnCl2 (cat.)
CH2Cl2, rt
Ph Ph
OMe
OMe
Ac
N
H
S
Ph
O
O O
Scheme 6. N-Acylation of sulfonamides with carboxylic acids in
the presence of ZnCl2 as a catalyst.
The arsenal of methods also contains the direct and mild
N-acylation of sulfonamides using esters as acylating agents
(Scheme 7). Several Lewis acids were studied as promoters,
among which TiCl4 proved to be the most effective,
affording high yields of the target N-acyl sulfonamides (up
to 97%). As in the previous examples, the simplicity of both
the reaction procedure and product isolation could be
highlighted [18].
N
H
S
R1
O
O
R2
O
NH2
S
R1
O
O
N
H
S
Tol
O
O
2Py
O
N
H
S
Tol
O
O
Tol
O
N
H
S
Tol
O
O
Ph
O
R2CO2R3
N
H
S
Me
O
O
Ph
O
97% 55% 45%
63%
TiCl4, (CHCl2)2,
115160 °C
S
CO2Et
NH2
O
O S
NH
O O
O82%
18 examples,
up to 97% yields,
R1, R2 = Ar, Alk;
R3 = Alk
N
H
S
Ph
O
O
Me
O
94%
N
H
S
Tol
O
O
Me
O
76%
Scheme 7. N-Acylation of sulfonamides with carboxylic esters in
the presence of TiCl4 (selected examples are given).
An interesting approach to the synthesis of N-acyl
sulfonamides employs cesium phosphotungstate
Cs5HP2W18O62 as an efficient and recyclable catalyst
(Scheme 8). This methodology is environmentally attractive
since the reactions are conducted in water using only
catalytic amounts of the reagent at rt. A variety of
representative N-acyl sulfonamides were synthesized in
high yields (up to 92%), whereas in refluxing water, cyclic
imides containing a sulfonyl fragment were formed [19].
N
S
Tol
O
O
R2
O
NH
S
Tol
O
O
N
H
S
Tol
O
O O
N
H
S
Tol
O
O O
N
H
S
Tol
O
O
Me
O
N
S
Tol
O
O
92% 90% 55%
77% 60%
N
S
Tol
O
O
Me
O
80%
Cs5HP2W18O62
(cat.), H2O, rt
CO2H
N
S
Tol
O
O
(R2CO)2O
R1 R1
33 examples.
up to 92% yields
R1, R2 = Ar, Alk
CO2H
O
O
O
O Br
Scheme 8. N-Acylation of sulfonamides with carboxylic
anhydrides in the presence of Cs5HP2W18O62 as a catalyst (selected
examples are given).
Another example of heterogeneous catalysis is the
application of iron-exchanged montmorillonite K10-FeO in
the N-acylation of sulfonamides with carboxylic anhydrides
ISSN 1814-9758. Ukr. Bioorg. Acta, 2025, Vol. 20, N 2
16
(Scheme 9), which was highly effective for a wide range of
sterically and electronically diverse substrates, providing
yields up to 98% and excellent chemoselectivity. As in the
previous case, the ability to reuse K10-FeO multiple times
without a significant loss of catalytic activity makes this
approach both economically and environmentally feasible
[20].
N
H
S
R1
O
O
R2
O
NH2
S
R1
O
O
N
H
S
Me
O
O
Me
O
N
H
S
Me
O
O
Ph
O
N
H
S
Ph
O
O
Me
O
92% 62% 82%
K10-FeO (cat.),
MeCN, 60 °C
(R2CO)2O 14 examples,
up to 98% yields
R1, R2 = Ar, Alk
N
H
S
O
O
CF3
O
N
H
S
O
O
Me
O
N
H
S
O
O
Me
O
98% 91% 66%
ClCl MeO
Scheme 9. N-Acylation of sulfonamides with carboxylic
anhydrides in the presence of K10-FeO (selected examples are
given).
A promising approach involves the use of metal
hydrogensulfates as acidic catalysts (Scheme 10). It has
been shown that Al(HSO4)3 and Zr(HSO4)4 exhibit the
highest activity in reactions of sulfonamides with
carboxylic anhydrides, efficiently catalyzing the process
under both heterogeneous and solvent-free conditions [21].
N
S
R1
O
O
R3
O
NH
S
R1
O
O
N
H
S
Me
O
O
Me
O
N
H
S
Ph
O
O
Me
O
Al(HSO4)3, neat, 90%
Al(HSO4)3, CH2Cl2, 91%
Zr(HSO4)4, neat, 93%
Zr(HSO4)4, CH2Cl2, 90%
Al(HSO4)3 or Zr(HSO4)4 (cat.),
CH2Cl2 or neat, rt
(R3CO)2O
>30 examples,
up to 96% yields
R1, R2 = Ar, Alk
Al(HSO4)3, neat, 88%
Al(HSO4)3, CH2Cl2, 86%
Zr(HSO4)4, neat, 96%
Zr(HSO4)4, CH2Cl2, 85%
N
S
Tol
O
O
Et
O
N
H
S
Tol
O
O
Et
O
Al(HSO4)3, neat, 92%
Al(HSO4)3, CH2Cl2, 88%
Zr(HSO4)4, neat, 89%
Zr(HSO4)4, CH2Cl2, 89%
Al(HSO4)3, neat, 75%
Al(HSO4)3, CH2Cl2, 75%
Zr(HSO4)4, neat, 72%
Zr(HSO4)4, CH2Cl2, 72%
R2 R2
Ph
Scheme 10. N-Acylation with carboxylic anhydrides in the
presence of Al(HSO4)3 or Zr(HSO4)4 (selected examples are
given).
N-Acylation of sulfonamides with carboxylic acids using
EDC (1-(3-dimethylaminopropyl)-3-ethylcarbodiimide) as a
typical activating reagent was also reported [22]. A more
advanced example involves the synthesis of an N-acyl
sulfonamide library using EDC immobilized on a polymer
support (Scheme 11). In this protocol, a sulfonic acid resin
(A-15) is employed to bind N,N-dimethylaminopyridine
(DMAP). The purification of the reaction mixture is
simplified to a simple filtration, making the method
convenient and suitable for large-scale applications. The
literature reports 25 examples of target product synthesis
using this method, with yields reaching up to 81% [23].
N
H
S
R1
O
O
Ph
O
NH2
S
R1
O
O
N
H
S
Bn
O
O
Ph
O
N
H
S
Ph
O
O
Ph
O
N
H
S
Me
O
O
Ph
O
66% 56% 64%
(CH2Cl)2, t-BuOH, DMAP,
PhCO2H,
25 examples,
up to 81% yields
R1, R2 = Ar, Alk
N
H
S
O
O
Ph
O
N
H
S
O
O
Ph
O
N
H
S
O
O
Ph
O
75% 63% 81%
O2N
N N
Cl-
C N
SO3H (A-15)
CO2Me Cl
Scheme 11. N-Acylation of sulfonamides with carboxylic acids in
the presence of EDC immobilized on polymer support (selected
examples are given).
A highly efficient and relatively mild approach relied on
the use of cyanuric chloride as an activating reagent of
carboxylic acid in the presence of triethylamine, and
aluminum oxide in acetonitrile at rt, to afford the target
products in yields of up to 92% (Scheme 12) [24].
N
H
S
R1
O
O
R2
O
NH2
S
R1
O
O
N
H
S
O
O
Tol
O
N
H
S
Me
O
O
Ph
O
N
H
S
Ph
O
O
Ph
O
92% 74% 55%
Et3N, Al2O3, MeCN, rt
16 examples,
up to 92% yields
R1, R2 = Ar, Alk
R2CO2H,
Cl
ClCl N
NN
BzHN
N
H
S
O
O
Me
O
N
H
S
Me
O
O
Me
O
N
H
S
Ph
O
O
Tol
O
85% 68% 60%
BzHN
Scheme 12. The straightforward synthesis using carboxylic acids
and cyanuric chloride (selected examples are given).
Another efficient approach involves the synthesis of N-
acyl sulfonamides through sequential reactions of primary
amines with arylsulfonyl chlorides followed by acylation of
the intermediates with acyl chlorides (Scheme 13).
In the first step, the reaction of anilines with arylsulfonyl
chlorides under solvent-free conditions in the presence of
O.V. Gavrylenko et al.
17
NaHCO3 leads to the formation of N-arylsulfonamides.
These intermediates are then subjected in situ to further
acylation with benzoyl chloride or its derivatives to afford
the corresponding N-benzoyl-N-arylsulfonamides.
Moreover, acylation of sulfonamides with acyl chlorides
can also be performed as a separate step (Scheme 14) [25].
N
S
R1
O
O
R3
O
S
R1
O
O
N
S
Tol
O
O
Ph
O
N
S
Tol
O
O
Ph
O
N
S
Ph
O
O
Ph
O
92% 86% 86%
2. R3C6H4COCl,
K2CO3, rt
Cl
R2
Ph oMeC6H4 oMeOC6H4
9 examples,
up to 96% yields
R1, R2 = Ar
N
S
Tol
O
O
Ph
O
N
S
Tol
O
O
Ph
O
N
S
Tol
O
O
Ph
O
72% 95% 96%
pMeOC6H4 mClC6H4 pClC6H4
1. R2NH2, NaHCO3,
rt, neat
Scheme 13. Sulfonylation and acylation as a one-pot method for
the synthesis of N-acyl sulfonamides (selected examples are
given).
N
S
R1
O
O
R3
O
S
R1
O
O
N
S
Tol
O
O
4-NO2C6H4
O
N
S
Ph
O
O
4-NO2C6H4
O
N
S
Ph
O
O
4-NO2C6H4
O
70% 80%
91%
K2CO3, rt, neat
R3C6H4COCl,
R2
NH
R2
Ph Tol
1-naphtyl
N
S
Tol
O
O
3,5-(NO2)2C6H4
O
N
S
Ph
O
O
3,5-(NO2)2C6H4
O
N
S
Ph
O
O
3,5-(NO2)2C6H4
O
84% 70%
95%
pClC6H4 Bn
oMeOC6H4
13 examples,
up to 95% yields
R1, R2, R3 = Ar
Scheme 14. N-Acylation of sulfonamides with carboxylic acid
chlorides in the presence of K2CO3 under solvent-free conditions
(selected examples are given).
An unusual approach to the synthesis of N-acyl
sulfonamides involves the use of air-stable and crystalline
N-acyl-DBN tetraphenylborate salts (1,5-diazabicyclo-
[4.3.0]-non-5-ene, Scheme 15), obtained from DBN and the
corresponding acyl chlorides in the presence of NaBPh4.
These salts act as efficient N-acylating agents that
selectively react with primary and secondary amines as well
as sulfonamides to give the desired products in high yields
of up to 98%. An advantage of this method is the ease of
product isolation, as the by-product DBN·HBPh4 can be
removed by simple filtration, providing pure N-acylated
compounds without the need for additional purification
steps. Notable, N-acyl-DBN tetraphenylborate salts can be
stored in air without the risk of decomposition [26].
N
S
R1
O
O
Me
O
S
R1 O
O
N
S
Tol
O
O
Me
O
N
H
S
Tol
O
O
Me
O
80%
65%
DBN (cat.),
MeCN, 80 °C
N
H
S
Ph
O
O
Me
O
83%
N
H
S
Me
O
O
Me
O
98%
R2
NH
R2
N
N
O Me
BPh4
-
N
H
S
O
O
Me
O
74%
MeO
Bn
Scheme 15. Application of N-acyl-DBN tetraphenylborate salts
for the synthesis of N-acyl sulfonamides.
Another approach to the synthesis of N-acyl
sulfonamides involves the use of N-acylbenzotriazoles
(R2COBt) as acylating agents, which could be beneficial in
the cases when the corresponding acyl chlorides or other
common acylating agents are difficult to access or unstable
(Scheme 16) [27].
N
H
S
R1
O
O
R2
O
NH2
S
R1 O
O
N
H
S
Tol
O
O
2-furyl
O
N
H
S
Tol
O
O
Tol
O
N
H
S
Tol
O
O
4-Py
O
R2COBt
N
H
S
Tol
O
O
4-Py
O
98%
95% 95% 97%
NaH, THF, reflux
Bt = benzotriazole
18 examples,
up to 100% yield
R1 = Ar, Alk; R2 = Ar;
R3 = Cbz, Ph, tBu
N
H
S
Me
O
O
Tol
O
92%
N
H
S
Me
O
O
2-furyl
O
98%
Scheme 16. N-Acylation of sulfonamides using N-acyl-
benzotriazoles (selected examples are given).
The reaction of sulfonamides was carried out with a wide
range of substrates in the presence of NaH in refluxing
THF. Additionally, it has been shown that N-sulfonyl-
benzotriazoles can participate in reactions with
carboxamide substrates as sulfonylating agents, providing
an alternative route to the target products (Scheme 17) [27].
The sulfonylation reactions will be discussed in more detail
in the following section.
N
H
S
R1
O
O
R2
O
Bt
S
R1 O
O
N
H
S
Tol
O
O
Tol
O
N
H
S
Tol
O
O
4-Py
O
R2CONH2
91%83%
NaH, THF, reflux
Bt = benzotriazole
N
H
S
Me
O
O
Tol
O
34%
N
H
S
Me
O
O
4-Py
O
77%
Scheme 17. N-Sulfonylation of carboxamides using N-sulfonyl-
benzotriazoles.
ISSN 1814-9758. Ukr. Bioorg. Acta, 2025, Vol. 20, N 2
18
An interesting example is an one pot reaction that uses
ZnO nanoparticles as heterogeneous catalyst (Scheme 18).
The reaction proceeds via sequential sulfonylation and
acylation of amines under solvent-free conditions,
providing high yields of up to 95% [28].
N
S
R1
O
O
R3
O
S
R1
O
O
N
H
S
Ph
O
O
Me
O
N
H
S
Me
O
O
Ph
O
N
H
S
Me
O
O
Me
O
X = AcO - 93%
X = Cl - 95%
X = Cl - 92% X = AcO - 91%
nano-ZnO (cat.),
2. R3COX
Cl
R2
15 examples,
up to 95% yields
R1, R2, R3 = Ar, Alk
N
S
Tol
O
O
Ph
O
N
S
Tol
O
O
Me
O
N
S
Me
O
O
Ph
O
X = Cl - 89% X = Cl - 93% X = Cl - 93%
Ph Ph nBu
1. R2NH2, rt
Scheme 18. Use of ZnO nanoparticles as a heterogeneous catalyst
for the synthesis of N-acyl sulfonamides (selected examples are
given).
N-Sulfonylation of amides
Another typical approach to the synthesis of N-acyl
sulfonamides involves sulfonylation reactions of
carboxamides.
N
S
Tol
O
O
R1
O
N
S
Tol
O
O
Me
O
N
H
S
Tol
O
O
Ph
O
N
H
S
Tol
O
O
Me
O
86% 85%
85%
EtOH/THF (2/1),
ultrasonic, rt
18 examples (5 of them
N-acyl sulfonamides),
up to 92% yieds
R1, R2 = Ar, Alk
N
S
Tol
O
O
Ph
O
83%
TolSO2Cl, Na
O
R1
NH
R2 R2
N N
S
O
O O
O
O
Tol
S
O
O
Tol
88%
Ph Ph
Scheme 19. N-Sulfonylation using pTsCl in the presence of Na in
EtOH–THF under ultrasonic conditions (selected examples are
given).
Another approach involves ultrasonic N-sulfonylation of
amines, imides, amides, and anilides using p-toluene-
sulfonyl chloride (pTsCl) in the presence of dispersed
sodium in an EtOH-THF mixture (Scheme 19). This
method combines robustness and high efficiency: the
reactions proceed under mild conditions, and are completed
within 2-8 minutes and afford high product yields of up to
92%. The protocol is also economically favorable due to the
use of readily available reagents, and the potential for scale-
up [29].
It is also worth noting that in cases where the amide
proton is sufficiently acidic, DMAP could be successfully
employed (Scheme 20) [30].
DMAP, MeCN, rt
74%
TolSO2Cl
NH
O
O
N
O
O
S
O
O
Tol
Scheme 20. N-Sulfonylation of amides in the presence of DMAP
as a mild base.
Synthesis from sulfonyl azides and isocyanates
An efficient one-step methodology for the conversion of
carboxylic acids into N-acyl sulfonamides via the reaction
with sulfonyl azides was reported (Scheme 21) [31].
N
H
S
R2
O
O
R1
O1. i-BuOCOCl,
2,6-lutidine, THF, 0 °C
N
H
S
O
O O
N
H
S
O
O O
N
H
S
O
O O
86% 83%
98%
N
H
S
O
O O
N
H
S
O
O O
96% 94%
R1 OH
O
2. TMS-SLi, THF, 0 °C
3. R2SO2N3
HO2C HO2C
HO2C
TMS TMS
OH
NHBoc
Me
OBn
Me
NHBoc
NHFmoc
Me
NHFmoc
Me
NHFmoc
NHBoc
R1 = Alk
R2 = Ar, Alk
Scheme 21. The conversion of carboxylic acids into N-acyl
sulfonamides via the formation of thioacids.
An intermediate step involves the formation of a
thioacid, which directly reacts with the sulfonyl azide to
afford the target products
A further development of this method included the use of
H2O/NMP (N-methyl-2-pyrrolidone) (1:3, v/v) in the pre-
sence of NaHCO3 at rt. The reaction was performed with
readily available thioacids and sulfonyl azides, allowing the
preparation of 18 examples in high yields (up to
quantitative) [32].
Other reports were devoted to the DNA-encoded libraries
(DEL), which is a typical approach in the drug discovery
programs. Considering the broad pharmacological relevance
of the N-acyl sulfonamide fragment, strategies enabling its
incorporation into DEL platforms have attracted particular
attention (Schemes 23 and 24).
The copper-catalyzed three-component reactions
between alkynes and sulfonyl azides efficiently generated
the diverse set of N-acyl sulfonamides in high yields (up to
96%) [33].
Another interesting transformation included the Pd(0)-
catalyzed carbonylative coupling of sulfonyl azides with
electron-rich heterocycles (Scheme 25).
O.V. Gavrylenko et al.
19
N
H
S
O
O
R2
O
N3
S
O
O
R2COSH
H2O/NMP (1/3),
NaHCO3, rt
18 examples,
up to 100% yields
R1, R2, R3 = Ar, Alk, H
H
N
R1
H
N
R1
N
H
S
O
O
Me
O
H2N
N
H
S
O
O
Ph
O
H2N
N
H
S
O
O
pCF3C6H4
O
H2N
90% 74%
100%
N
H
S
O
O
Me
O
H
N
Ac
N
H
S
O
O
pNO2C6H4
O
H
N
Ac
N
H
S
O
O
oMeOC6H4
O
H
N
Ac
91%
84% 90%
Scheme 22. The reaction of sulfonyl azides into N-acyl
sulfonamides (selected examples are given).
HN
S
R1
O
O
ON3
S
R1 O
O
CuI, DIPEA, DMF
borate buffer, rt
20 examples, up to 96% yield, R1 = Ar, Alk
83% 73% 83%
96% 65% 69%
HN
O
DNA HN
O
DNA
N
N
N
N
CF3
N
N
BrNO2
CF3 O
O
Scheme 23. Copper-catalyzed three-component reaction of
sulfonyl azides and alkynes integrated into DNA-encoded libraries
(selected examples are given).
The key step involves the in situ formation of a sulfonyl
isocyanate intermediate from the corresponding sulfonyl
azide, followed by regioselective C-C bond formation of
indole or pyrrole nucleophiles. This approach enabled the
synthesis of more than 35 examples of indole- and pyrrole-
substituted N-acyl sulfonamides in yields of up to 95%. The
method does not require the use of specialized ligands, is
compatible with an ex situ solid CO source and operates
under mild conditions (40 °C). An additional advantage of
this protocol is the possibility of isotopic labeling of N-acyl
sulfonamides with carbon-11, making it particularly
attractive for subsequent biological evaluation and in vivo
studies using positron emission tomography (PET) [34].
The literature also reports the direct use of aryl sulfonyl
isocyanates in reactions with carboxylic acids to afford
N-acyl sulfonamides (Scheme 26). The reaction proceeds
efficiently in THF at rt in the presence of Et3N and is
accompanied by CO2 evolution. A few minutes after the gas
release ceases, the corresponding N-acyl sulfonamides were
formed in high yields [35].
NH
S
O
O
O
CuI, DIPEA, DMF
borate buffer, rt
15 examples, up to 73% yields, R1 = Ar
73% 57%
51% 41%
S
HN
O
DNA
R1
N
OMe
CF3
R1
O
N3 O
O
DNA
48%
58%
60%
53%
tBu
NO2
OMe
OMe
S
Scheme 24. Variation of the copper-catalyzed three-component
reaction between alkynes and sulfonyl azides integrated into
DNA-encoded libraries (selected examples are given).
N
H
S
R1
O
O O
N3
S
R1 O
O
Pd(OAc)2 (cat.), CO,
N
H
S
Tol
O
O
O
68%
Mo(CO)6, DBU,
MeCN, N2, 40 °C N
R3
N
R3
R2
R2
>35 examples, up to 95% yields, R1, R2, R3 = Ar, Alk, H
N
Ph
N
H
S
Tol
O
O
O
84%
N
Me
N
H
S
Bun
O
O
O
70%
N
Me
Ph
N
H
S
O
O
O
89%
N
Me
S
N
H
S
Tol
O
O
O
76%
N
N
H
S
Tol
O
O
O
84%
N
Me
Ph
Scheme 25. Palladium(0)-catalyzed synthesis of N-acyl
sulfonamides (selected examples are given).
ISSN 1814-9758. Ukr. Bioorg. Acta, 2025, Vol. 20, N 2
20
N
H
S
R1
O
O
R2
O
S
R1
N
H
S
Tol
O
O
O
97%
10 examples,
up to 100% yields
R1, R2 = Ar, Alk
N
H
S
Tol
O
O
O
96%
N
H
S
Tol
O
O
O
85%
N
H
S
Tol
O
O
O
100% 83%
90%
NCO
O
O
R2
O
HO
CO2Me
Br
Me
Me
O
N
H
O
S
Me
O
O
O
N
H
O
S
Tol
O
O
NEt3
THF, rt
Scheme 26. Synthesis of N-acyl sulfonamides from sulfonyl
isocyanates and carboxylic acids (selected examples are given).
Miscellaneous synthetic methods
The photocatalytic synthesis of N-acyl sulfonamides was
also reported (Scheme 27). The reaction is based on
S-N coupling between sodium sulfinates and hydroxamic
acids or N-hydroxycarbamates in the presence of the
photocatalyst 2,3,5,6-tetra(9H-carbazol-9-yl)benzonitrile
(4CzBN). This method enables access to a broad range of
target sulfonamides in high yields of up to 97%.
Mechanistic investigations confirmed that the key step
involves the generation of singlet oxygen (1O2) through an
energy transfer process [36].
The reaction of N-sulfonyl-1,2,3-triazoles with thioesters
in the presence of a rhodium(II) catalyst also provides
access to N-acyl sulfur-containing sulfonamides in a
stereoselective manner (Scheme 28). The mechanism of this
transformation involves the formation of an α-imino
rhodium carbene complex, followed by nucleophilic attack
of the sulfur atom of thioester on the carbene carbon and
intramolecular migration of the acyl group from sulfur to
the imino nitrogen [37]. Notably, this approach was also
successfully employed for the synthesis thiolactones.
The related approach included the reaction of N-sulfonyl-
1,2,3-triazoles with thioesters in the presence of a rhodium
catalyst. However, in this case, the use of acyl selenides
instead of thioesters enables the formation of N-acyl
selenium-containing sulfonamides as the target products
(Scheme 29). The reaction proceeds upon heating and in the
presence of the Rh2Piv4 complex, which catalyzes a rapid
and stereoselective 1,3-difunctionalization. The high
functional group tolerance of this method was confirmed in
35 examples, with yields reaching up to 95% [38].
Copper catalysis has opened a new direction in the
reactivity of nitrones and enamides, enabling the diversion
of classical thermal dipolar cycloadditions toward the
formation of γ-keto- and γ-aldoamides (Scheme 30). The
key step involves the generation of an iminium intermediate
resulting from the nucleophilic attack of the activated
enamide. This initiates a diastereoselective rearrangement
accompanied by the formation of a new C-C bond, where
the alkyne group of the N-alkynyl sulfonamide is
transformed into an acyl group, leading to the target N-acyl
sulfonamides in high yields of up to 98% [39].
N
H
S
R1
O
O
R2
O
S
R1
N
H
S
Tol
O
O
2-OHC6H4
O
33%
>30 examples,
up to 97% yield
R1 = Ar, Alk; R2 = Ar, OR
N
H
S
Tol
O
O
O
52%
N
H
S
O
O
4-tBuC6H4
O
92%
N
H
S
Tol
O
O
4-FC6H4
O
84% -
97%
ONa
O
4CzBN (cat.),
Na2S2O4, BTAC
R2
O
N
H
4-tBuC6H4N
H
O
S
Et
O
O
N
H
O
S
Tol
O
O
iPrOAc/H2O/AcOH,
blue light, rt
HO
N
N
N
N
N
4CzBN
S
Scheme 27. Photocatalytic synthesis of N-acyl sulfonamides from
sodium sulfinates and hydroxamic acids or N-hydroxycarbamates
(selected examples are given).
>20 examples,
up to 95% yields
R1, R2, R3, R4 = Ar, Alk
[(tBuCO2)4Rh2]
(cat.), CHCl3
R3
O
S 4A mol sieves,
70 °C
N
N
N
S
O
O
R2
R1 R4 N
S
O
O
R2R1
R3
S
R4 O
H H
N
S
O
O
Tol
Tol
Me
S
Ph O
H
N
S
O
O
Tol
Me
S
Ph O
H
N
S
O
O
Me
Ph
Me
S
Ph O
H
N
S
O
O
t-Bu
Ph
Me
S
Ph O
H
N
S
O
O
Tol
Ph
Me
S
Et O
H
N
S
O
O
Tol
Ph
Ph
S
Ph O
H
N
S
O
O
Tol
Ph
Me
S
Ph O
H
N
S
O
O
TolPh
O
S
H
95% 89%
80% 78% 86%
67% 78% 84%
NHBoc
Scheme 28. Reaction of triazoles with thioesters leading to N-acyl
sulfur-containing sulfonamides (selected examples are given).
O.V. Gavrylenko et al.
21
>40 examples, up to 95% yields, R1, R2, R3 = Ar, Alk
Rh2Piv4 (cat.)
R2
O
Se PhMe, 100 °C
N
N
N
S
O
O
R1
Ar1 R3 N
S
O
O
R1Ar1
R2
Se
R3 O
H H
N
S
O
O
Tol
Tol
Me
Se
Ph O
H
N
S
O
O
Tol
Me
Se
Ph O
H
N
S
O
O
Tol
Ph
Bn
Se
Ph O
H
N
S
O
O
pCNC6H4
Ph
Me
Se
Ph O
H
N
S
O
O
Tol
Ph
Me
Se
Ph O
H
N
S
O
O
i-PrPh
O
Ph Se
H
95% 95% 63%
69% 95% 57%
Me
S
Scheme 29. Synthesis of N-acyl selenium-containing sulfonamides
via Rh-catalyzed reaction of triazoles with acyl selenides (selected
examples are given).
15 examples, up to 98% yields, R1, R2, R3, R4, R5 = Ar, Alk, H
Cu(OTf)2/AgBF4
(cat.)
SiO2, (CH2Cl)2, rt
R3
N
R2
S
O
N R2
S
O
O
R1
85% 95%
87%
O
N
O
R5
R4
R1
N
N
O
R3
R4
R5
O
N
Ph
S
O
O
Tol
O
O
N
Ph
S
O
O
Tol
O
Ph
O
Et
N
Ph
S
O
O
Tol
O
O
N
Boc
98% 81%
72% (dr >20/1)
N
Ph
S
O
O
Tol
O
O
N
Me
S
O
O
Me
O
Ph
O
Et
N
Me
S
O
O
Tol
O
H
O
Ph
O O
Scheme 30. Copper-catalyzed synthesis of N-acyl sulfonamides
from N-alkynyl sulfonamides (selected examples are given).
Finally, another interesting approach involves the
transacylation of N-acyl sulfonamides. The described study
proposes a general method for FeCl3-catalyzed trans-
acylation, in which acetic anhydride serves as the new
acylating agent (Scheme 31). The dual role of FeCl3 relies
in the simultaneous catalysis of the non-hydrolytic
deacylation and subsequent re-acylation of the formed
sulfonamide. In addition to FeCl3, GaCl3 and RuCl3·xH2O
were also shown to be good catalysts [40].
Conclusions
The multitude of synthetic methods available for N-acyl
sulfonamide construction underscores the versatility and
importance of this functional group in organic and
N
S
R1
O
O
Me
O
S
R1
O
O
97% 96% 94%
Ac2O (access), rtN
>20 examples,
up to 99% yields
R1, R2 = Ar, Alk;
R3 = Ar, Alk, H
99% 91% 93%
R2
O
FeCl3 (cat.)
S
Tol
O
O
N
H
1-naphtyl
O
S
Ph
O
O
N
H
n-Bu
O
S
Bn
O
O
N
H
n-Bu
O
S
Tol
O
O
N
O
S
Tol
O
O
N t-Bu
O
S
Me
O
O
N t-Bu
O
R3 R3
Bn Me Ph
Scheme 31. FeCl3-catalyzed transacylation of N-acyl sulfon-
amides (selected examples are given).
medicinal chemistry. Classical acylation techniques
(reacting sulfonamides with acyl chlorides or anhydrides)
remain the common solutions for straightforward cases,
offering simplicity and high yields.
At the same time, newer catalytic approaches address more
demanding synthetic scenarios. For instance, the use of
heterogeneous and reusable acid catalysts (silica-supported
phosphates, heteropoly acids, modified clays, etc.) has
enabled greener, solvent-free or aqueous protocols without
compromising efficiency. Many of these catalyst systems
can be recycled multiple times, aligning with principles of
sustainability while still delivering N-acyl sulfonamides in
good to excellent yields.
The ability to carry out one-pot sulfonylation-acylation
sequences further streamlines synthesis by avoiding
intermediate isolation. Notably, some recently developed
protocols can produce the target compounds in a matter of
minutes under very mild conditions (e.g. ultrasound-
promoted sulfonylations).
In addition to improving traditional routes, cutting-edge
methodologies have expanded the chemical space of N-acyl
sulfonamides. The integration of sulfonyl azide in copper-
catalyzed multicomponent reactions and palladium-
catalyzed carbonylations allow the incorporation of N-acyl
sulfonamide motifs into complex molecular frameworks,
e.g., azoles, or even DNA-linked substrates.
Overall, the field of N-acyl sulfonamide synthesis has
evolved, where researchers can choose from an extensive
toolkit of methods to suit their specific substrate
requirements, functional group compatibilities, and
environmental considerations. As further improvements in
catalytic methods and novel reaction paradigms emerge,
one can expect the synthesis of N-acyl sulfonamides to
become even more streamlined, adaptable, and suitable for
the parallel syntheses, thereby accelerating the discovery
and development of new therapeutic agents decorated with
this functional group.
Notes
Acknowledgments. The authors thank all the brave
defenders of Ukraine that stood against the russian full-
scale invasion and made this publication possible.
ISSN 1814-9758. Ukr. Bioorg. Acta, 2025, Vol. 20, N 2
22
The authors declare no conflict of interest.
Author contributions. The manuscript was written
through contributions of all authors. All authors have given
approval to the final version of the manuscript.
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https://go.drugbank.com/
O.V. Gavrylenko et al.
23
Синтез N-ацилсульфонамідів: від загальновідомих реакцій ацилювання
до сучасних каталітичних і сталих методів
О.В. Гавриленко1, Б.С. Сосунович1, Б. В. Ващенко2,3*, О.О. Григоренко1,2,3, Ю.С. Мороз1,3,4
1 ТОВ НВП «Єнамін» (www.enamine.net), Київ, Україна
2 Київський національний університет імені Тараса Шевченка, Київ, Україна
3 Науково-дослідний інститут (НДІ) «Єнамін», Київ, Україна
4 ТОВ "Кемспейс", Київ, Україна
Резюме: N-Ацилсульфонаміди є широко застосовуваними біоізостерами карбонових кислот, цінними завдяки сприятливим фізико-хімічним та
фармакокінетичним властивостям і поширеному використанню у структурах лікарських засобів. У цьому огляді узагальнено основні синтетичні
підходи до цих сполук, охоплюючи як класичні, так і новітні методи з акцентом на каталітичні, екологічні та прості у виконанн і підходи.
Найпоширеніші методи включають безпосереднє N-ацилювання сульфонамідів та N-сульфонілювання карбоксамідів, а також перетворення за
участі сульфонілазидів, сульфонілізоціанатів і споріднених багатокомпонентних процесів. Останні розробки полягають у застосув анні
гетерогенних каталізаторів, здатних до регенерування та багаторазового використання, водних розчинів або проведння реакцій без розчинника, а
також у застосуванні реакцій карбонілювання, фотокаталітичних реакцій утворення зв'язків S-N та перетворення за участю перехідних металів,
які підкреслюють простоту та ефективність підходів. Ці досягнення формують адаптивний і ефективний інструментарій для синтезу
різноманітних N-ацилсульфонамідів, важливих для сучасної органічної та медичної хімії.
Ключові слова: N-ацилсульфонаміди; зелена хімія; каталіз; біоізостери.
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| id | oai:ojs2.bioorganica.com.ua:article-103 |
| institution | Ukrainica Bioorganica Acta |
| keywords_txt_mv | keywords |
| language | English |
| last_indexed | 2026-06-30T01:00:22Z |
| publishDate | 2025 |
| publisher | V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine |
| record_format | ojs |
| resource_txt_mv | bioorganicacomua/10/0739365bea1c907244698df5bd799e10.pdf |
| spelling | oai:ojs2.bioorganica.com.ua:article-1032026-06-29T15:59:56Z Synthesis of N-acyl sulfonamides: from common acylation reactions to modern catalytic and sustainable methods Синтез N-ацилсульфонамідів: від загальновідомих реакцій ацилювання до сучасних каталітичних і сталих методів Gavrylenko, Oleksii V. Sosunovych, Bohdan S. Vashchenko, Bohdan V. Grygorenko, Oleksandr O. Moroz, Yurii S. N-acyl sulfonamides green chemistry catalysis bioisosteres N-ацилсульфонаміди зелена хімія каталіз біоізостери N-Acyl sulfonamides are widely used bioisosteres of carboxylic acids, valued for their favorable physicochemical and pharmacokinetic properties as well as their frequent occurrence in drug-like molecules. This review summarizes the principal synthetic approaches to these motifs, covering both established and emerging methodologies, with emphasis on catalytic, green, and operationally simple approaches. Common strategies include direct N-acylation of sulfonamides and N-sulfonylation of carboxamides, as well as transformations employing sulfonyl azides, sulfonyl isocyanates, and related multicomponent processes. Recent developments, such as recyclable heterogeneous catalysts, solvent-free and aqueous conditions, carbonylative and photocatalytic S-N couplings, and mild transition-metal-mediated reactions highlight simplicity and sustainability. Collectively these advances provide an adaptable and efficient synthetic toolbox for accessing diverse N-acyl sulfonamides relevant to modern organic and medicinal chemistry. N-Ацилсульфонаміди є широко застосовуваними біоізостерами карбонових кислот, цінними завдяки сприятливим фізико-хімічним та фармакокінетичним властивостям і частому використанню у структурах лікарських засобів. У цьому огляді узагальнено основні синтетичні підходи до цих сполук, охоплюючи як класичні, так і новітні методи з акцентом на каталітичні, екологічні та прості у виконанні підходи. Найпоширеніші методи включають безпосереднє N-ацилювання сульфонамідів та N-сульфонілювання карбоксамідів, а також перетворення за участі сульфонілазидів, сульфонілізоціанатів і споріднених багатокомпонентних процесів. Останні розробки полягають у застосуванні гетерогенних каталізаторів, здатних до регенерування та багаторазового використання, водних розчинів або проведння реакцій без розчинника, а також у застосуванні реакцій карбонілювання, фотокаталітичних реакцій утоврення зв'язків S-N та перетворення за участі перехідних металів, які підкреслюють простоту та ефективність підходів. Ці досягнення формують адаптивний і ефективний інструментарій для синтезу різноманітних N-ацилсульфонамідів, важливих для сучасної органічної та медичної хімії. V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine 2025-12-31 Article Article application/pdf https://bioorganica.com.ua/index.php/journal/article/view/103 10.15407/bioorganica2025.02.013 Ukrainica Bioorganica Acta; Vol. 20 No. 2 (2025): Ukrainica Bioorganica Acta; 13-23 Ukrainica Bioorganica Acta; Том 20 № 2 (2025): Ukrainica Bioorganica Acta; 13-23 1814-9766 1814-9758 10.15407/bioorganica2025.02 en https://bioorganica.com.ua/index.php/journal/article/view/103/100 Copyright (c) 2025 Oleksii V. Gavrylenko, Bohdan S. Sosunovych, Bohdan V. Vashchenko, Oleksandr O. Grygorenko https://creativecommons.org/licenses/by/4.0 |
| spellingShingle | N-ацилсульфонаміди зелена хімія каталіз біоізостери Gavrylenko, Oleksii V. Sosunovych, Bohdan S. Vashchenko, Bohdan V. Grygorenko, Oleksandr O. Moroz, Yurii S. Синтез N-ацилсульфонамідів: від загальновідомих реакцій ацилювання до сучасних каталітичних і сталих методів |
| title | Синтез N-ацилсульфонамідів: від загальновідомих реакцій ацилювання до сучасних каталітичних і сталих методів |
| title_alt | Synthesis of N-acyl sulfonamides: from common acylation reactions to modern catalytic and sustainable methods |
| title_full | Синтез N-ацилсульфонамідів: від загальновідомих реакцій ацилювання до сучасних каталітичних і сталих методів |
| title_fullStr | Синтез N-ацилсульфонамідів: від загальновідомих реакцій ацилювання до сучасних каталітичних і сталих методів |
| title_full_unstemmed | Синтез N-ацилсульфонамідів: від загальновідомих реакцій ацилювання до сучасних каталітичних і сталих методів |
| title_short | Синтез N-ацилсульфонамідів: від загальновідомих реакцій ацилювання до сучасних каталітичних і сталих методів |
| title_sort | синтез n-ацилсульфонамідів: від загальновідомих реакцій ацилювання до сучасних каталітичних і сталих методів |
| topic | N-ацилсульфонаміди зелена хімія каталіз біоізостери |
| topic_facet | N-acyl sulfonamides green chemistry catalysis bioisosteres N-ацилсульфонаміди зелена хімія каталіз біоізостери |
| url | https://bioorganica.com.ua/index.php/journal/article/view/103 |
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