Strain-release arylations for the bis-functionalization of azetidines.

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 N Ar reactions or Buchwald-Hartwig couplings.