The development of a continuous flow process to the synthesis of GSK2395675B demontrated on Vapourtec instruments is described. Borate reagents screening has been carried out and the suitable tributyl borate is identified to resolve the clogging issue due to the gel formation when lithiated intermediate reacts with pinacol borate. Key benefits in the continuous process include the elimination of the cryogenic conditions required in the batch process, and the cost reduction (10 times) in borate reagents by utilizing tris-butyl borate instead of pinacol borate. In addition, new process understandings on the borylation stage are discussed.

Development of a continuous flow process to manage GSK2251052A stage 4 exothermic chemistry

248th National Meeting (2014)

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