Synthesis of triazolo-fused benzoxazepines and benzoxazepinones via Passerini reactions followed by 1,3-dipolar cycloadditions

Mol Divers. 2014 Aug;18(3):473-82. doi: 10.1007/s11030-014-9530-x. Epub 2014 Jun 4.

Abstract

Azidobenzaldehydes can be used in Passerini three-component condensations to synthesize small collections of triazolo-fused heterocycles in an efficient and combinatorial fashion upon post-condensation azide-alkyne cycloadditions. Triazolo-fused benzoxazepinones were obtained in moderate to good overall yields with a concise two-step protocol. Triazolo-fused benzoxazepines were instead prepared by means of a longer, yet straightforward route comprising a Passerini reaction, hydrolysis of the ester moiety, O-alkylation with propargylic bromides, and 1,3-dipolar cycloaddition.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Benzoxazines / chemical synthesis*
  • Benzoxazines / chemistry*
  • Cycloaddition Reaction*
  • Hydrolysis
  • Triazoles / chemistry*

Substances

  • Benzoxazines
  • Triazoles