Cu-Catalyzed Cyanation of Indoles with Acetonitrile as a Cyano Source

J Org Chem. 2015 Sep 4;80(17):8868-73. doi: 10.1021/acs.joc.5b01419. Epub 2015 Aug 26.

Abstract

Cu-catalyzed cyanation of indoles with acetonitrile for the synthesis of 3-cyanoindoles has been developed. The Cu/TEMPO/(Me3Si)2 system has been identified to promote highly efficient and selective C-H cyanation of indoles by use of unactivated acetonitrile as a cyano source via a sequential iodination/cyanation process in one pot. This reaction furnishes 3-cyanoindoles in moderate to good yields and tolerates a series of functional groups. Moreover, low-cost copper catalysts and hazardless acetonitrile as a cyano source feature the practicability of this reaction.

Publication types

  • Research Support, Non-U.S. Gov't