Journal
ORGANIC PROCESS RESEARCH & DEVELOPMENT
Volume 14, Issue 1, Pages 168-173Publisher
AMER CHEMICAL SOC
DOI: 10.1021/op900260k
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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.
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