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Difluoro-Substituted Bicyclo[1.1.1]pentanes for Medicinal Chemistry: Design, Synthesis, and Characterization

2019; American Chemical Society; Volume: 84; Issue: 23 Linguagem: Inglês

10.1021/acs.joc.9b01947

1520-6904

Roman Bychek, Valeriia Hutskalova, Yuliya P. Bas, Olga A. Zaporozhets, Sergey Zozulya, Vadym V. Levterov, Pavel K. Mykhailiuk,

Synthesis and Reactions of Organic Compounds

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.