Organic Chemistry

Difluoro-Substituted bicyclo[1.1.1]pentanes as Novel Motifs for Medicinal Chemistry: Design, Synthesis and Characterization


Herein we developed a practical synthetic approach to the previously unknown difluoro-substituted bicyclo[1.1.1]pentanes. The key step was an addition of difluorocarbene to electron-rich bicyclo[1.1.0]butanes by CF3TMS/NaI system. The obtained difluoro-bicyclo[1.1.1]pentanes are a new generation of saturated bioisosteres of the benzene ring for drug discovery projects.


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Supplementary material

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190716 SI