Strain-release arylations for the bis-functionalization of azetidines

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 S_NAr reactions or Buchwald–Hartwig couplings.