Jean-Paul Kestemont, J. Frost, J. Jacq
May 19, 2021
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Influential Citations
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Journal
Organic Process Research & Development
Abstract
We report a large-scale carboxylation of N-Boc-4,4-difluoropiperidine (1) enabled by a continuous flow process. The flow process involved N-Boc-directed α-deprotonation using s-BuLi in THF and subsequent trapping with CO2 gas. Flow chemistry enabled the safe and scalable preparation of 400 g of carboxylic acid 2 over the course of a day to support our medicinal chemistry research program.