Regioselective Base-Mediated Cyclizations of Mono-N-acylpropargylguanidines

J Org Chem. 2017 Jul 7;82(13):6958-6967. doi: 10.1021/acs.joc.7b00639. Epub 2017 Jun 15.

Abstract

A regioselective base-mediated cyclization of mono-N-acylpropargylguanidines is reported. A related Ag(I)-catalyzed hydroamination strategy was recently employed to yield N3-Cbz-protected ene-guanidines, which found utility in the synthesis of naamidine A. Herein, we report the base-catalyzed hydroamination of mono-N-acylpropargylguanidines, which proceeds with the opposite regiochemistry to deliver isomerized N2-acyl-2-aminoimidazoles with broad substrate scope, circumventing the problematic regiospecific acylation of free 2-aminoimidazoles.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Cyclization
  • Guanidines / chemistry*
  • Molecular Structure
  • Spectrum Analysis / methods
  • Stereoisomerism

Substances

  • Guanidines