C-N Cross-Couplings for Site-Selective Late-Stage Diversification via Aryl Sulfonium Salts

J Am Chem Soc. 2019 Aug 28;141(34):13346-13351. doi: 10.1021/jacs.9b07323. Epub 2019 Aug 14.

Abstract

We report diverse C-N cross-coupling reactions of aryl thianthrenium salts that are formed site-selectively by direct C-H functionalization. The scope of N-nucleophiles ranges from primary and secondary alkyl and aryl amines to various N-containing heterocycles, and the overall transformation is applicable to late-stage functionalization of complex, drug-like small molecules.

Publication types

  • Research Support, Non-U.S. Gov't