One-Pot Synthesis of Multifunctionalized 1-Pyrrolines from 2-Alkyl-2 H-azirines and Diazocarbonyl Compounds

J Org Chem. 2022 Jul 1;87(13):8835-8840. doi: 10.1021/acs.joc.2c00977. Epub 2022 Jun 22.

Abstract

A novel strategy for the synthesis of 1-pyrrolines based on formal [4 + 1] annulation of 2-alkyl-2H-azirines with diazocarbonyl compounds has been developed. This one-pot approach includes the Rh(II)-catalyzed formation of 4-alkyl-2-azabuta-1,3-dienes, followed by the DBU-promoted cyclization, and features a good substrate tolerance. The 1-pyrrolines containing an ester group at the C3 were prepared in a three-step one-pot procedure starting from 5-alkoxyisoxazoles. The cyclization of 2-azabutadienes to 1-pyrrolines most likely proceeds via the 6π electrocyclization of a conjugated NH-azomethine ylide.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Azirines* / chemistry
  • Catalysis
  • Cyclization

Substances

  • Azirines