Discovery and Development of an Efficient, Scalable, and Robust Route to the Novel CENP-E Inhibitor GSK923295A

R Bellingham, AM Buswell, BM Choudary…

Index: Bellingham, Richard; Buswell, A. Mark; Choudary, Bernie M.; Gordon, Andrew H.; Moore, Steve O.; Peterson, Matthew; Sasse, Mike; Shamji, Amin; Urquhart, Michael W. J. Organic Process Research and Development, 2010 , vol. 14, # 5 p. 1254 - 1263

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Citation Number: 5

Abstract

The discovery and development of an efficient manufacturing route to the CENP-E inhibitor 3- chloro-N-{(1 S)-2-[(N, N-dimethylglycyl) amino]-1-[(4-{8-[(1 S)-1-hydroxyethyl] imidazo [1, 2- a] pyridin-2-yl} phenyl) methyl] ethyl}− 4-[(1-methylethyl) oxy] benzamide (GSK923295A) is described. The existing route to GSK923295A was expensive, nonrobust, used nonideal reagents, and consistently struggled to deliver the API needed for clinical studies. The ...