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Development of a safe and efficient continuous flow method for the synthesis of 3-difluoromethoxypyridine derivatives

Lehmann, Hansjoerg, Ruppen, Thomas, Oswald, Susanne, Ye, Ning, Tian, Xiangguang, Dai, Chunhui and Fairhurst, Robin (2025) Development of a safe and efficient continuous flow method for the synthesis of 3-difluoromethoxypyridine derivatives. Helvetica chimica acta, 108 (e20240). ISSN 1522-2675

Abstract

The development of a safe, efficient and scalable continuous-flow-chemistry protocol for the O-difluoromethylation of two 3-hydroxypyridine building blocks is described. This example highlights that continuous flow chemistry has become firmly established within Novartis Biomedical Research, and when implemented appropriately can enable the continuous supply of material from the first realization of a potentially interesting intermediate within a discovery project all the way through to clinical evaluation.

Item Type: Article
Keywords: difluoromethylation, continuous flow chemistry, exothermic reaction, DFF332, scale-up
Date Deposited: 26 Apr 2025 00:45
Last Modified: 26 Apr 2025 00:45
URI: https://oak.novartis.com/id/eprint/55795

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