Copper-Catalyzed Oxidative Dearomatization/Spirocyclization of Indole-2-Carboxamides: Synthesis of 2-Spiro-pseudoindoxyls

Org Lett. 2016 Dec 2;18(23):6124-6127. doi: 10.1021/acs.orglett.6b03131. Epub 2016 Nov 14.

Abstract

A copper-catalyzed oxidative dearomatization/spirocyclization of indole-2-carboxamides using tert-butyl hydroperoxide (TBHP) as the oxidant has been developed that provides rapid and efficient access to C2-spiro-pseudoindoxyls. Two of the sp2 C-H bonds are functionalized during the reaction process, and the reaction likely proceeds via the formation of a highly reactive 3H-indol-3-one intermediate followed by aromatic electrophilic substitution with the N-aryl ring of the amide moiety.

Publication types

  • Research Support, Non-U.S. Gov't