Ruthenium-Catalyzed Synthesis of 2H-Azirines from Isoxazolinones

Org Lett. 2017 Sep 1;19(17):4436-4439. doi: 10.1021/acs.orglett.7b01895. Epub 2017 Aug 23.

Abstract

2H-Azirines are synthetically versatile, highly strained, three-membered heterocycles containing an imino double bond. We report their efficient Ru-catalyzed synthesis using low catalyst loadings under neutral conditions from isoxazolinone substrates, which are readily accessible from β-ketoesters. The azirines were shown to be efficient precursors for functionalized pyridine, indole, dihydropyrrole, and pyrrolidine heterocycles.

Publication types

  • Research Support, Non-U.S. Gov't