4.8 Article

Palladium-Catalyzed Dehydrogenative Fluoroalkoxylation of Benzaldehydes

Journal

ORGANIC LETTERS
Volume 23, Issue 5, Pages 1921-1927

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.1c00365

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Funding

  1. National Natural Science Foundation of China [NSFC-21572178, NSFC-21702162, NSFC-21971206]

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An efficient palladium-catalyzed oxidative dehydrogenative fluoroalkoxylation of benzaldehydes is reported with mild reaction conditions and good functional group tolerance. The method employs a transient directing group strategy, avoiding the need for additional installation and removal of directing groups, making it economically advantageous with great potential for applications in drug synthesis and discovery processes.
A direct and efficient palladium-catalyzed oxidative dehydrogenative fluoroalkoxylation of benzaldehydes is reported here for the first time. The method features mild reaction conditions, good tolerance of functional groups, and a broad substrate scope. The protocol employs the transient directing group strategy, thereby avoiding the additional installation and removal of directing groups, endowing the method with great advantages of atom and step economy. The approach should find broad applications in drug synthesis and discovery processes.

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