Modular and Stereoselective Approach to Highly Substituted Indole/Pyrrole-Fused Diazepanones

J Org Chem. 2021 May 7;86(9):6458-6466. doi: 10.1021/acs.joc.1c00303. Epub 2021 Apr 28.

Abstract

A one-pot synthetic method for indole/pyrrole-fused 1,4-diazepanone scaffolds has been developed. This method involves a sequential amide coupling/intramolecular aza-Michael addition of 1H-indole/pyrrole-2-carboxylic acids with Morita-Baylis-Hillman-derived allylamines. The readily available starting materials, good stereoselectivity, and gram-scale synthesis make this method valuable for the construction of highly substituted fused heterocycles containing the 1,4-diazepanone moiety.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Indoles*
  • Molecular Structure
  • Pyrroles*
  • Stereoisomerism

Substances

  • Indoles
  • Pyrroles