Rhodium-Catalyzed Site-Selective Coupling of Indoles with Diazo Esters: C4-Alkylation versus C2-Annulation

Org Lett. 2017 Nov 17;19(22):6184-6187. doi: 10.1021/acs.orglett.7b03099. Epub 2017 Nov 7.

Abstract

A Rh(III)-catalyzed site-selective C-H activation of C(3)-functionalized indoles in a coupling with diazo esters has been realized with carbonyl as a weakly coordinating group. The coupling selectivity is dictated by the temperature and additives, affording either C4-alkylated indoles or C2-annulated lactones in moderate to excellent efficiency.

Publication types

  • Research Support, Non-U.S. Gov't