Issue 39, 2021

Recent strategies used in the synthesis of saturated four-membered heterocycles

Abstract

The importance and prevalance of O-, N-, and S-atom containing saturated four-membered ring motifs in biologically active molecules and potential therapeutics continues to drive efforts in their efficient synthetic preparation. In this review, general and recent strategies for the synthesis of these heterocycles are presented. Due to the limited potential bond disconnections, retrosynthetic strategies are broadly limited to cyclizations and cycloadditions. Nonetheless, diverse approaches for accessing cyclization precursors have been developed, ranging from nucleophilic substitution to C–H functionalization. Innovative methods for substrate activation have been developed for cycloadditions under photochemical and thermal conditions. Advances in accessing oxetanes, azetidines, and thietanes remain active areas of research with continued breakthroughs anticipated to enable future applications.

Graphical abstract: Recent strategies used in the synthesis of saturated four-membered heterocycles

Article information

Article type
Review Article
Submitted
22 svi 2021
Accepted
13 ruj 2021
First published
13 ruj 2021

Org. Biomol. Chem., 2021,19, 8425-8441

Author version available

Recent strategies used in the synthesis of saturated four-membered heterocycles

K. P. Malarney, S. KC and V. A. Schmidt, Org. Biomol. Chem., 2021, 19, 8425 DOI: 10.1039/D1OB00988E

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