Synthesis of benzoxazoles via an amine-catalyzed [4 + 1] annulation

Org Lett. 2013 May 17;15(10):2510-3. doi: 10.1021/ol400988e. Epub 2013 May 8.

Abstract

An unprecedented simple pyrrolidine catalyzed [4 + 1] annulation reaction of ynals with N-protected-2-aminophenols is reported. The utilization of the unique property and reactivity of the C≡C triple bond in ynals leads to two consecutive conjugate addition reactions at the same β-position with pyrrolidine via iminium activation. The powerful cascade process affords a new alternative approach to biologically and synthetically important benzoxazoles in high yields (83-95%).

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Amines / chemistry*
  • Benzoxazoles / chemical synthesis*
  • Benzoxazoles / chemistry
  • Catalysis
  • Imines / chemistry
  • Molecular Structure
  • Pyrrolidines / chemistry*

Substances

  • Amines
  • Benzoxazoles
  • Imines
  • Pyrrolidines
  • pyrrolidine