Ruthenium(II)-Catalyzed Site-Selective Hydroxymethylation of Indolines with Paraformaldehyde

J Org Chem. 2019 Feb 15;84(4):2307-2315. doi: 10.1021/acs.joc.8b02873. Epub 2018 Dec 19.

Abstract

The facile synthesis of hydroxymethylated indole derivatives is crucial for their further development as pharmaceutical compounds and other synthetic purposes. Herein, we describe the ruthenium(II)-catalyzed hydroxymethylation of indolines and other N-heterocycles using paraformaldehyde as an abundant C1 feedstock. A wide substrate scope range and high levels of site selectivity as well as functional group tolerance were observed.

Publication types

  • Research Support, Non-U.S. Gov't