二氟取代的二环[1.1.1]戊烷在药物化学中的设计、合成与表征。
Difluoro-Substituted Bicyclo[1.1.1]pentanes for Medicinal Chemistry: Design, Synthesis, and Characterization.
机构信息
Enamine Ltd. , Chervonotkatska 78 , Kyiv 02094 , Ukraine.
Taras Shevchenko National University of Kyiv , Chemistry Department , Volodymyrska 64 , Kyiv 01601 , Ukraine.
出版信息
J Org Chem. 2019 Dec 6;84(23):15106-15117. doi: 10.1021/acs.joc.9b01947. Epub 2019 Oct 7.
PMID:31553875
Abstract
A practical synthetic approach to the difluoro-substituted bicyclo[1.1.1]pentanes was developed. The key step was an addition of difluorocarbene (:CF) to electron-rich bicyclo[1.1.0]butanes by the CFTMS/NaI system. The obtained difluoro-bicyclo[1.1.1]pentanes are suggested to be used as saturated bioisosteres of benzene rings for the purpose of drug discovery projects.
摘要
开发了一种实用的二氟取代双环[1.1.1]戊烷的合成方法。关键步骤是通过 CFTMS/NaI 体系将二氟卡宾 (:CF) 加成到富电子的双环[1.1.0]丁烷上。所得到的二氟双环[1.1.1]戊烷被建议用作苯环的饱和生物等排体，用于药物发现项目。
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