Investigation of Synthetic Routes to a Key Benzopyran Intermediate of a 5HT4 Agonist

…, NG Stevenson, NR Curtis, JM Northall…

Index: Stevenson, Neil G.; Curtis, Neil R.; Northall, John M.; Gray, Matthew; Prodger, Jeremy C.; Walker, Andrew J. Organic Process Research and Development, 2010 , vol. 14, # 1 p. 92 - 98

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Citation Number: 16

Abstract

The supply route to GlaxoSmithKline's 5HT4 receptor agonist 1 centred on the construction of key benzopyran fragment 2. Our attempts to define the final manufacturing route for this component are described through a series of disconnections. The systematic approach undertaken towards the construction of the benzopyran skeleton focused on cyclisation strategies from appropriate precursors and evaluation of the performance of the key steps.