Synthesis of Five-Membered Cyclic Guanidines via Cascade [3 + 2] Cycloaddition of α-Haloamides with Organo-cyanamides

J Org Chem. 2021 Feb 19;86(4):3546-3554. doi: 10.1021/acs.joc.0c02932. Epub 2021 Feb 4.

Abstract

The convenient preparation of N2-unprotected five-membered cyclic guanidines was achieved through a cascade [3 + 2] cycloaddition between organo-cyanamides and α-haloamides under mild conditions in good to excellent yields (up to 99%). The corresponding cyclic guanidines could be easily transformed into hydantoins via hydrolysis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cyanamide*
  • Cycloaddition Reaction
  • Guanidine
  • Guanidines*
  • Hydrolysis

Substances

  • Guanidines
  • Cyanamide
  • Guanidine