Recent advances in the late-stage modification of complex bioactive molecules with oxetanes and azetidines
Abstract
Oxetanes and azetidines have emerged as increasingly prominent motifs in medicinal chemistry, offering compact, polar frameworks that finely modulate the physicochemical properties of drug candidates. The selective late-stage incorporation of these highly strained, C(sp 3 )-rich heterocycles into complex bioactive molecules opens exciting new chemical space and allows practitioners to focus on core scaffold design rather than the synthetic challenges intrinsic to these unique ring systems. This Minireview highlights recent advances in the late-stage modification of complex bioactive molecules with oxetane and azetidine units, featuring representative studies reported between 2022 and 2025.
Fields of Study & Subjects
Synthesis and Catalytic Reactions
Chemical Synthesis and Analysis
Radical Photochemical Reactions
Publication details
- Journal / source
- Tetrahedron Chem
- Publisher
- Elsevier BV
- Volume
- 17
- Pages
- 100153–100153
- Publication date
- 10 January 2026
- Language
- EN