Development of a manufacturing process for sibenadet hydrochloride, the active ingredient of Viozan

…, AJG Morlin, J Tornos, S Atkinson, C Just…

Index: Giles, Melvyn E.; Thomson, Colin; Eyley, Stephen C.; Cole, Andrea J.; Goodwin, Christopher J.; Hurved, Paul A.; Morlin, Andrew J. G.; Tornos, James; Atkinson, Stephanie; Just, Cecelia; Dean, Janet C.; Singleton, John T.; Longton, Andrew J.; Woodland, Ian; Teasdale, Andrew; Gregertsen, Bjoern; Else, Howard; Athwal, Mandip S.; Tatterton, Stephen; Knott, Jason M.; Thompson, Nicola; Smith, Stephen J. Organic Process Research and Development, 2004 , vol. 8, # 4 p. 628 - 642

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Citation Number: 20

Abstract

A process for commercial manufacture of the dual D2-β2 receptor agonist sibenadet hydrochloride has been developed. The process relies upon introduction of operationally simple chemistry at the final stages where two key intermediates are reacted to assemble the final molecule, isolated by crystallization. A nine-stage sequence for synthesis of the key amine hydrochloride intermediate was developed, and modifications to the original ...