4-Membered Ring Carbocations: A Positive Development in the Synthesis of 3,3-Disubstituted Oxetanes and Azetidines

Juan J. Rojas; James A. Bull

doi:10.2533/chimia.2023.192

4-Membered Ring Carbocations: A Positive Development in the Synthesis of 3,3-Disubstituted Oxetanes and Azetidines

Authors

Juan J. Rojas Department of Chemistry, Imperial College London, W12 0BZ London https://orcid.org/0000-0002-9471-5888
James A. Bull Department of Chemistry, Imperial College London, W12 0BZ London https://orcid.org/0000-0003-3993-5818

DOI:

https://doi.org/10.2533/chimia.2023.192

Keywords:

Azetidines, Bioisosteres, Carbocations, Chemical Space, Oxetanes

Abstract

4-Membered heterocycles are low molecular weight polar scaffolds with intriguing potential for drug discovery. Despite their unquestionable value, methods to access such heterocycles remain scant. Here, we describe the generation of oxetane- and azetidine- benzylic carbocations as a general strategy to access valuable 3,3-disubstituted derivatives.