Improved Synthesis of the Selective Rho-Kinase Inhibitor 6-Chloro-N 4-{3, 5-difluoro-4-[(3-methyl-1 H-pyrrolo [2, 3-b] pyridin-4-yl) oxy] phenyl} pyrimidin-2, 4-diamine

H Schirok, H Paulsen, W Kroh, G Chen…

Index: Schirok, Hartmut; Paulsen, Holger; Kroh, Walter; Chen, Gang; Gao, Ping Organic Process Research and Development, 2010 , vol. 14, # 1 p. 168 - 173

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Citation Number: 8

Abstract

A highly potent and selective Rho-kinase inhibitor containing a 7-azaindole moiety has been developed at Bayer Schering Pharma. Herein we disclose details of a significantly improved synthesis of the compound in 8.2% overall yield. Key aspects include cost and safety considerations and the uncommon use of a trifluoromethyl group with controllable reactivity as a masked methyl group.