Journal
ORGANIC LETTERS
Volume 21, Issue 20, Pages 8205-8210Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.9b02887
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- Sanofi [8091314]
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Here, we report a general method for the synthesis of quaternary and tertiary difluoromethylated compounds and their vinylfluoride analogues. The strategy, which relies on a two-step sequence featuring a C-selective electrophilic difluoromethylation and either a palladium-catalyzed decarboxylative protonation or a Krapcho decarboxylation, is practical, scalable, and high yielding. 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.
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