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金催化的后MCR反应向复杂(多)杂环的转化。

Gold-catalyzed post-MCR transformations towards complex (poly)heterocycles.

作者信息

Sharma Upendra K, Tian Guilong, Voskressensky Leonid G, Van der Eycken Erik V

机构信息

Laboratory for Organic & Microwave-Assisted Chemistry (LOMAC), Department of Chemistry, University of Leuven (KU Leuven), Celestijnenlaan 200F, B-3001, Leuven, Belgium.

Peoples Friendship University of Russia (RUDN University), Miklukho-Maklaya Street 6, 117198 Moscow, Russia.

出版信息

Drug Discov Today Technol. 2018 Nov;29:61-69. doi: 10.1016/j.ddtec.2018.08.003. Epub 2018 Aug 28.

Abstract

Post multicomponent reaction (MCR) transformations are one of the most successful methods leading to high structural diversity and molecular complexity. A well-known MCR, the Ugi reaction typically affords a linear peptide backbone, enabling post-Ugi transformations as an elegant solution to rigidify the Ugi adduct into more drug-like species. Not surprisingly, the development of such transformations leading to new structural frameworks has expanded rapidly over the last few years. These reactions have reached an impressive level of performance and versatility, particularly in amalgamation with gold catalysis. This review outlines the developments achieved in the past decade, highlighting the modifications that are performed in a sequential or domino fashion with emphasis on major concepts, synthetic applications of the derived products as well as mechanistic aspects.

摘要

多组分反应(MCR)后的转化是产生高结构多样性和分子复杂性的最成功方法之一。著名的MCR反应——乌吉反应通常能提供线性肽骨架,使乌吉反应后的转化成为将乌吉加合物刚性化为更具药物样性质物种的优雅解决方案。毫不奇怪,在过去几年中,导致新结构框架的此类转化的发展迅速。这些反应在性能和通用性方面达到了令人印象深刻的水平,特别是与金催化结合时。本综述概述了过去十年所取得的进展,重点介绍了以连续或多米诺方式进行的修饰,着重阐述主要概念、衍生产品的合成应用以及机理方面。

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