Sequential C-Selective Difluoromethylation/Pd-Catalyzed Decarboxylative Protonation: An Efficient Access to Tertiary Difluoromethylated Scaffolds

08 May 2019, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

We report here a general method that allows a highly straightforward access to tertiary difluoromethylated compounds. The strategy relies on a two-step sequence featuring a C-selective electrophilic difluoromethylation and an unprecedented palladium-catalyzed decarboxylative protonation. Considering the generality of the method and the attractive properties offered by the difluoromethyl group, this approach provides a valuable tool for late-stage functionalization and drug development.

Keywords

difluoromethylation
Pd-catalysed decarboxylative protonation
lactams
lactones
Late-stage functionalization

Supplementary materials

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