Selective One-Pot Cascade Synthesis of N-Substituted Highly Functionalized Pyrroles from Unprotected Sugars, Primary Amines, and Oxoacetonitriles

J Org Chem. 2022 Sep 16;87(18):12115-12131. doi: 10.1021/acs.joc.2c01270. Epub 2022 Aug 31.

Abstract

A one-pot, three-component cascade reaction between unprotected sugars, primary amines, and 3-oxoacetonitriles gave N-substituted 2,3,5-functionalized pyrroles or N-substituted 2,3,4-functionalized pyrroles in excellent yields and selectivities. The selectivity of the reaction was achieved by simple control of the sequence of substrate addition. The reaction showed a wide substrate scope, and various types of sugars, primary amines, and oxoacetonitriles reacted smoothly. The work demonstrates a highly desired simple reaction for embedding nitrogen into sugars to produce valuable N-heterocyclic compounds that are amenable to further modifications to natural products and drug intermediates.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amines / chemistry
  • Biological Products*
  • Catalysis
  • Heterocyclic Compounds* / chemistry
  • Nitrogen
  • Pyrroles / chemistry
  • Sugars

Substances

  • Amines
  • Biological Products
  • Heterocyclic Compounds
  • Pyrroles
  • Sugars
  • Nitrogen