I2-mediated regioselective C-3 azidation of indoles

Org Biomol Chem. 2016 Mar 21;14(11):3027-30. doi: 10.1039/c6ob00295a. Epub 2016 Feb 25.

Abstract

An unprecedented synthesis of novel 3-azido indoles has been developed using I2 and NaN3 in high yields and excellent regioselectivity. The reaction proceeds under metal-free conditions at room temperature. Essentially, an umpolung in reactivity at the C-3 position of indole has been achieved by the activation of indoles with I2.

Publication types

  • Research Support, Non-U.S. Gov't