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

preprint
submitted on 08.05.2019 and posted on 08.05.2019 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.

History

Email Address of Submitting Author

s.arseniyadis@qmul.ac.uk

Institution

Queen Mary University of London

Country

United Kingdom

ORCID For Submitting Author

0000-0001-6831-2631

Declaration of Conflict of Interest

The authors declare no competing financial interest

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