Взаємодія N-(трет-бутилсульфініл)іміну трифторопірувату з діазометаном як зручний синтетичний підхід до енантіомерних трифторометиламінокислот

The interaction of enantiomerically pure N-tert-butylsulfinyl imines of trifluoropyruvate with diazomethane has been studied. It has been shown that there is the [3+2]-cycloaddition at the initial step with the formation of diastereomeric trifluoromethyltriazoline carboxylates in the ratio of 5.6:1....

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Збережено в:
Бібліографічні деталі
Дата:2025
Автори: Zakharko, Roman M., Rassukana, Yuliya V.
Формат: Стаття
Мова:Англійська
Опубліковано: National University of Pharmacy 2025
Теми:
Онлайн доступ:https://ophcj.nuph.edu.ua/article/view/343956
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Назва журналу:Journal of Organic and Pharmaceutical Chemistry

Репозитарії

Journal of Organic and Pharmaceutical Chemistry
Опис
Резюме:The interaction of enantiomerically pure N-tert-butylsulfinyl imines of trifluoropyruvate with diazomethane has been studied. It has been shown that there is the [3+2]-cycloaddition at the initial step with the formation of diastereomeric trifluoromethyltriazoline carboxylates in the ratio of 5.6:1. Treating the triazoline carboxylates with trifluoroacetic acid yielded optically pure aziridine carboxylates, which were subsequently converted into their corresponding acids. When subjected to hydrochloric acid in an ethereal solution, trifluoromethylaziridines underwent ring-opening and the sulfinyl group removal, producing α-chloromethylamino acids. The study also demonstrates the potential use of these aziridinecarboxylic acids in the peptide synthesis.