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

页码：168 / 173

页数：6

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