Difluoro-Substituted Bicyclo[1.1.1]pentanes for Medicinal Chemistry: Design, Synthesis, and Characterization
Difluoro-Substituted Bicyclo[1.1.1]pentanes for Medicinal Chemistry: Design, Synthesis, and Characterization
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DOI：
10.1021/acs.joc.9b01947
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发表时间：
2019-12-06
影响因子：
3.6
通讯作者：
Mykhailiuk, Pavel K.
中科院分区：
文献类型：
--
作者：
Bychek, Roman M.;Hutskalova, Valeriia;Mykhailiuk, Pavel K.
发展了一种合成二氟取代双环[1.1.1]戊烷的实用方法。关键步骤是通过CF_3TMS/NaI体系将二氟卡宾（：CF_2）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]戊烷可作为苯环的饱和生物电子等排体用于药物发现项目。
A practical synthetic approach to the difluoro-substituted bicyclo[1.1.1]pentanes was developed. The key step was an addition of difluorocarbene (:CF2) to electron-rich bicyclo[1.1.0]butanes by the CF3TMS/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.