Selection and development of the manufacturing route for EP1 antagonist GSK269984B

M Whiting, K Harwood, F Hossner…

Index: Whiting, Matthew; Harwood, Kathy; Hossner, Frank; Turner, Peter G.; Wilkinson, Mark C. Organic Process Research and Development, 2010 , vol. 14, # 4 p. 820 - 831

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Citation Number: 12

Abstract

A potential manufacturing route for the EP1 antagonist GSK269984B was developed. Four synthetic approaches were examined, and a successful realisation of each is presented. The rationale supporting selection of the preferred route is discussed. This route utilised a phenolic aldol reaction as the key step and relied on selective hydrogenolysis to reduce an intermediate diarylmethanol. Further optimisation of the selected route is presented, ...