Affiliation:
1. Graduate School of Life Sciences Tohoku University 2-1-1 Katahira Aoba-ku Sendai Japan
Abstract
AbstractIn contrast to the considerable progress in the development of methodologies for amide bond formation in amines, the development of direct N‐acylation of less nucleophilic N‐heterocycles and amides with carboxylic acids is still challenging. In this report, we describe the direct N‐acylation of less nucleophilic heterocycles and amides with carboxylic acids promoted by the 4‐(N,N‐dimethylamino)pyridine N‐oxide (DMAPO)/di‐tert‐butyl dicarbonate (Boc2O) system. The new one‐pot method, which does not involve pre‐activation of substrates, enables the direct N‐acylation of a wide variety of nitrogen nucleophiles such as indole, carbazole, pyrrole, pyrazole, lactam, oxazolidinone, and anilide with carboxylic acids in high yield. The new method also exhibits excellent functional group tolerance and broad substrate scope. As the present method is practical, operationally simple, and scalable, it should find wide applications in both academic and industrial laboratories.
Subject
Inorganic Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Catalysis
Cited by
4 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献