Taming 3-Oxetanyllithium Using Continuous Flow Technology.

ABSTRACT: The oxetane ring has evolved as a useful bioisostere for dimethyl and carbonyl groups for the improvement of physiochemical properties of drug candidates. Herein, we report the generation and utilization of highly unstable 3-oxetanyllithium as a hitherto unexplored nucleophile leveraging flash technology. A range of different electrophiles are suitable reaction partners in this protocol, and we demonstrate the utility of this protocol in late-stage pharmaceutical analogue synthesis.

SUBMITTER: Natho P 

PROVIDER: S-EPMC11041934 | biostudies-literature | 2024 Apr

REPOSITORIES: biostudies-literature