Harnessing Oxetane and Azetidine Sulfonyl Fluorides for Opportunities in Drug Discovery.

ABSTRACT: Four-membered heterocycles such as oxetanes and azetidines represent attractive and emergent design options in medicinal chemistry due to their small and polar nature and potential to significantly impact the physiochemical properties of drug molecules. The challenging preparation of these derivatives, especially in a divergent manner, has severely limited their combination with other medicinally and biologically important groups. Consequently, there is a substantial demand for mild and effective synthetic strategies to access new oxetane and azetidine derivatives and molecular scaffolds. Here, we report the development and use of oxetane sulfonyl fluorides (OSFs) and azetidine sulfonyl fluorides (ASFs), which behave as precursors to carbocations in an unusual defluorosulfonylation reactio

SUBMITTER: Symes OL 

PROVIDER: S-EPMC11673132 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature