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Copper-Catalyzed Synthesis of 5-Carboxyl-4-perfluoroalkyl Triazoles

Robert Panish*, Tho Thieu and Jaume Balsells

*Discovery Process Research, Janssen R&D, 1400 McKean Road, Spring House, Pennsylvania 19477, United States, Email: rpanishits.jnj.com

R. Panish, T. Thieu, J. Balsells, Org. Lett., 2021, 23, 5937-5941.

DOI: 10.1021/acs.orglett.1c02037


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Abstract

Copper catalyzes a rapid assembly of 5-carboxyl-4-perfluoroalkyl-triazoles from N-tosylhydrazides and perfluoroalkyl acetoacetates. The approach exhibits high functional group tolerance and can be executed on a multigram scale.

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Key Words

1,2,3-triazoles, DMSO


ID: J54-Y2021