Synthetic Approaches to Contemporary Drugs that Contain the Cyclopropyl Moiety,Synthesis

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Synthetic Approaches to Contemporary Drugs that Contain the Cyclopropyl Moiety
Synthesis ( IF 2.2 ) Pub Date : 2020-03-16 , DOI: 10.1055/s-0039-1690058
Zdenko Časar _{1,

2}

Affiliation

The U.S. Food and Drug Administration approved 18 new drugs that incorporate the cyclopropyl structural motif in the time frame from 2012 to 2018. This review provides an overview of synthetic approaches to these drugs with emphasis on the construction of the cyclopropyl moiety or its incorporation into the key building blocks for assembly of the highlighted drugs. Based on the structural diversity of these drugs, synthetic approaches for the construction and introduction of the cyclopropyl moiety into their structure are diverse and include: cycloalkylation (double alkylation) of CH-acids, catalytic cyclopropanation of alkenes with diazo compounds, the Simmons–Smith reaction, the Corey–Chaykovsky reaction, the Kulinkovich reaction, the Horner–Wadsworth–Emmons reaction, and cycloaddition. In addition, the cyclopropyl structure was also introduced into the drug substance intermediates via simple cyclopropyl-moiety-containing building blocks, such as cyclopropylamine, cyclopropanesulfonamide, cyclopropanecarbonyl chloride, and cyclopropylmagnesium bromide.

中文翻译：

包含环丙基部分的当代药物的合成方法

美国食品和药物管理局（FDA）批准了18种在2012年至2018年期间纳入环丙基结构基序的新药。该综述概述了这些药物的合成方法，重点是环丙基部分的结构或将其结合到药物中。突出药物组装的关键组成部分。基于这些药物的结构多样性，用于构建环丙基部分并将其引入结构的合成方法也多种多样，包括：CH酸的环烷基化（双烷基化），烯烃与重氮化合物的催化环丙烷化，Simmons–Smith反应，Corey–Chaykovsky反应，Kulinkovich反应，Horner–Wadsworth–Emmons反应和环加成反应。此外，

更新日期：2020-03-19

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