A Broad-Spectrum, Catalytic Amidation of Sulfonyl Fluorides and Fluorosulfates

19 October 2020, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

A broad-spectrum, catalytic amidation has been developed to prepare various sulfonamides and sulfamates including sterically hindered ones. In addition, the potentials of this methodology in medicinal and process chemistry have been demonstrated by the multidecagram-scale synthesis of an amantadine derivative and the synthesis of the marketed drug Fedratinib for myelofibrosis.

Keywords

SuFEx reaction
sterically hindered
sulfonamides
sulfamates
nucleophilic catalyst
organocatalysis

Supplementary materials

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SI-chemrxiv-LL
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