- 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
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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.
- Schirok, Hartmut,Paulsen, Holger,Kroh, Walter,Chen, Gang,Gao, Ping
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scheme or table
p. 168 - 173
(2010/04/29)
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- Substituted Phenylamino-Pyrimidines
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The invention relates to substituted phenylaminopyrimidines, to a process for their preparation and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases in humans and animals, in particular cardiovascular disorders.
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- HETARYLOXY-SUBSTITUTED PHENYLAMINO PYRIMIDINES AS RHO KINASE INHIBITORS
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The invention relates to hetaryloxy-substituted phenylamino pyrimidines, a method for the production thereof, and the use thereof for producing medicaments utilized for the treatment and/or prevention of diseases in humans and animals, particularly cardiovascular diseases.
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Page/Page column 15
(2010/02/14)
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- SUBSTITUTED PHENYLAMINO-PYRIMIDINES
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The invention relates to substituted phenylamino-pyrimidines, to a method for their production and to their use for producing medicaments for the treatment and/or prophylaxis of diseases in humans and animals, in particular for the treatment of cardiovascular diseases.
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Page/Page column 27-28
(2010/02/14)
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- HETEROARYLOXY-SUBSTITUTED PHENYLAMINOPYRIMIDINES AS RHO-KINASE INHIBITORS
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The invention relates to heteroaryloxy-substituted phenylaminopyrimidines, to methods for the production thereof, and to the use of the same for producing medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular diseases. The inventive compounds inhibit Rho-kinase.
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Page/Page column 64
(2010/02/06)
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- Synthesis of 4-Amino-1H-pyrrolopyridine (1,7-Dideazaadenine) and 1H-Pyrrolopyridin-4-ol (1,7-Dideazahypoxanthine)
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4-Amino-1H-pyrrolopyridine (1,7-dideazaadenine) (5) has been synthesized by the iron and acetic acid reduction of 4-nitro-1H-pyrrolopyridine 7-oxide (13), obtained by nitration of 1H-pyrrolopyridine-3-carboxamide 7-oxide (17).Other nitration reactions in the 1H-pyrrolopyridine 7-oxide series are disclosed.The preparation of 1H-pyrrolopyridin-4-ol (1,7-dideazahypoxanthine) (6) began with the hydrolysis of ethyl 1-benzyl-3-cyano-4-oxo-4,7-dihydro-1H-pyrrolopyridine-5-carboxylate (21) to the 3,5-dicarboxylic acid derivative of 1-benzyl-4-oxo-4,7-dihydro-1H-pyrrolopyridine (22).Decarboxylation of 22 with subsequent debenzylation formed 6.
- Schneller, Stewart W.,Luo, Jiann-Kuan
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p. 4045 - 4048
(2007/10/02)
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