Strain-release arylations for the bis-functionalization of azetidines

Chem Commun (Camb). 2022 Feb 17;58(15):2564-2567. doi: 10.1039/d1cc07053c.

Abstract

The addition of nucleophilic organometallic species onto in situ generated azabicyclobutanes enables the selective formation of 3-arylated azetidine intermediates through strain-release. Single pot strategies were further developed for the N-arylation of resulting azetidines, employing either SNAr reactions or Buchwald-Hartwig couplings.