Improved Synthesis of the Selective Rho-Kinase Inhibitor 6-Chloro-N4-{3,5-difluoro-4-[(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl}pyrimidin-2,4-diamine

被引：13
作者：
Schirok, Hartmut [1 ]
Paulsen, Holger [1 ]
Kroh, Walter [1 ]
Chen, Gang [2 ]
Gao, Ping [2 ]
机构：
[1] Bayer Schering Pharma AG, Med Chem Wuppertal, D-42096 Wuppertal, Germany
[2] Chinese Acad Sci, Shanghai Inst Organ Chem, Shanghai 200032, Peoples R China
来源：
ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2010年 / 14卷 / 01期
关键词：
EMBRYONIC STEM-CELLS; VASCULAR SMOOTH-MUSCLE; ANEURYSMAL SUBARACHNOID HEMORRHAGE; POTENTIAL THERAPEUTIC TARGET; ORGANIC FLUORINE-COMPOUNDS; BINDING PROTEIN RHO; POSTMARKETING SURVEILLANCE; CARDIOVASCULAR-DISEASES; MYOSIN PHOSPHATASE; ROCK INHIBITORS;
D O I：
10.1021/op900260k
中图分类号：
O69 [应用化学];
学科分类号：
081704 ;
摘要：
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.
引用
收藏
页码：168 / 173
页数：6
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