Difluoro-Substituted Bicyclo[1.1.1]pentanes for Medicinal Chemistry: Design, Synthesis, and Characterization.
J Org Chem
; 84(23): 15106-15117, 2019 12 06.
Article
em En
| MEDLINE
| ID: mdl-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 (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.
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MEDLINE
Idioma:
En
Ano de publicação:
2019
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Article