Intramolecular Ring-Opening Decomposition of Aryl Azetidines

ACS Med Chem Lett. 2021 Sep 30;12(10):1585-1588. doi: 10.1021/acsmedchemlett.1c00402. eCollection 2021 Oct 14.

Abstract

The ring strain present in azetidines can lead to undesired stability issues. Herein, we described a series of N-substituted azetidines which undergo an acid-mediated intramolecular ring-opening decomposition via nucleophilic attack of a pendant amide group. Studies were conducted to understand the decomposition mechanism enabling the design of stable analogues.