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

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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… Click to show full 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.

Keywords: strain release; release arylations; arylations bis; functionalization azetidines; bis functionalization

Journal Title: Chemical communications
Year Published: 2022

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