Електрофільні реакції 7-(трифлуорометил)-2,3-дигідро-1H-піролізину – шлях до нових будівельних блоків

Aim. To synthesize new fluoro-containing building blocks for medicinal chemistry purposes using electrophilic reactions of 7-(trifluoromethyl)-2,3-dihydro-1H-pyrrolizine.Results and discussion. Synthetic approaches to 5-halogeno- and 5-acyl-7-(trifluoromethyl)-2,3-dihydro-1H-pyrrolizines have been d...

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Bibliographic Details
Date:2023
Main Authors: Klipkov, Anton A., Gerus, Igor I.
Format: Article
Language:English
Published: National University of Pharmacy 2023
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Online Access:https://ophcj.nuph.edu.ua/article/view/284640
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Journal Title:Journal of Organic and Pharmaceutical Chemistry

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Journal of Organic and Pharmaceutical Chemistry
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Summary:Aim. To synthesize new fluoro-containing building blocks for medicinal chemistry purposes using electrophilic reactions of 7-(trifluoromethyl)-2,3-dihydro-1H-pyrrolizine.Results and discussion. Synthetic approaches to 5-halogeno- and 5-acyl-7-(trifluoromethyl)-2,3-dihydro-1H-pyrrolizines have been developed. The obtained new trifluoromethyl-containing pyrrolyzines are promising building blocks for medicinal chemistry.Experimental part. The synthesis of the target compounds began with known 7-(trifluoromethyl)-2,3-dihydro-1H-pyrrolizine and included halogenation and acylation reactions using N-halogen succinimides and acylating reagents.Conclusions. New synthetic approaches to a number of 7-(trifluoromethyl)-2,3-dihydro-1H-pyrrolizines with various substituents, such as halogen atoms or acyl groups, at the position 5 of the pyrrole ring have been developed. This opens the door to the use of such promising trifluoromethyl-containing building blocks for medicinal chemistry needs.