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

Strain-release arylations for the bis-functionalization of azetidines

Florian Trauner  1 , Felix Reiners  1 , Kodjo-Edmond Apaloo-Messan  2 , Benedikt Nißl  1 , Muhammad Shahbaz  1 , Dongfang Jiang  1 , Julian Aicher  1 , Dorian Didier  1
Affiliations

Strain-release arylations for the bis-functionalization of azetidines

Florian Trauner et al. Chem Commun (Camb). .

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.

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