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

submitted on 08.05.2019, 02:32 and posted on 08.05.2019, 17:06 by Nicolas Duchemin, Roberto Buccafusca, Marc Daumas, Vincent Ferey, Stellios Arseniyadis
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.


Email Address of Submitting Author


Queen Mary University of London


United Kingdom

ORCID For Submitting Author


Declaration of Conflict of Interest

The authors declare no competing financial interest