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Reductive Cleavage of Secondary Sulfonamides: Converting Terminal Functional Groups into Versatile Synthetic Handles

preprint
submitted on 01.10.2019 and posted on 03.10.2019 by Patrick Fier, Suhong Kim, Kevin M. Maloney
Sulfonamides are pervasive in drugs and agrochemicals, yet are typically considered as terminal functional groups rather than synthetic handles. To enable the general late-stage functionalization of secondary sulfonamides, we have developed a mild and general method to reductively cleave the N-S bonds of sulfonamides to generate sulfinates and amines, components which can further react in-situ to access a variety of other medicinally relevant functional groups. The utility of this platform is highlighted by the selective manipulation of several complex bioactive molecules.

History

Email Address of Submitting Author

patrick.fier@merck.com

Institution

Merck & Co., Inc.

Country

USA

ORCID For Submitting Author

0000-0002-6102-815X

Declaration of Conflict of Interest

N/A

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