The Synthesis of Bromomethyltrifluoroborates through Continuous Flow Chemistry

Simon A Watson, Andrew Rutter,Malcolm Berry, Ben Hagger, Gary Lacking,Ranjit Chima, Graeme Marchbank, Gareth Alford,Paul Evans, Christopher Cunningham, John C Roberts,Robert B Perni, Toby Broom, Mark Jason Hughes,Bruce Szczepankiewicz, Karl Ace

Organic Process Research & Development(2014)

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摘要
A continuous flow process was developed for the synthesis of potassium bromomethyltrifluoroborate, a key precursor for SuzukiMiyaura coupling reagents. The continuous flow process was used to produce potassium bromomethyltrifluoroborate on scales from grams to kilograms, and the successful process utilized a fraction of the resources required for the batch synthesis. In the plant, a team of three people produced approximately 100 kg of potassium bromomethyltrifluoroborate in less than 4 weeks. This process makes it both practical and economical to use potassium bromomethyltrifluoroborate and its derivatives for multikilogram-scale SuzukiMiyaura couplings.
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