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Updated: Jun 29, 2025

Continuous Flow Chemistry: Reaction of Diphenyldiazomethane with p-Nitrobenzoic Acid
Published on: November 15, 2017
Taming 3-Oxetanyllithium Using Continuous Flow Technology
Philipp Natho1, Marco Colella1, Michael Andresini1
1FLAME-Lab, Flow Chemistry and Microreactor Technology Laboratory, Department of Pharmacy-Drug Sciences, University of Bari "A. Moro", Via E. Orabona 4, 70125, Bari, Italy.
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.

