Suzuki-Miyaura approach to JNJ-26076713, an orally active tetrahydroquinoline-containing alphaVbeta3/alphaVbeta5 integrin antagonist. enantioselective synthesis and stereochemical studies

An improved scale-up synthesis was required for the alpha(V)beta(3)/alpha(V)beta(5) integrin antagonist 1, which had demonstrated oral efficacy in eye disease models of angiogenesis and vascular permeability. A stereodefined, quinoline-substituted, unsaturated ester was conveniently prepared by a Su...

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Veröffentlicht in:	Journal of organic chemistry 2008-03, Vol.73 (6), p.2302-2310
Hauptverfasser:	Kinney, William A, Teleha, Christopher A, Thompson, Andrew S, Newport, Maria, Hansen, Ryan, Ballentine, Scott, Ghosh, Shyamali, Mahan, Andrew, Grasa, Gabriela, Zanotti-Gerosa, Antonio, Dingenen, Jules, Schubert, Carsten, Zhou, Yong, Leo, Gregory C, McComsey, David F, Santulli, Rosemary J, Maryanoff, Bruce E
Format:	Artikel
Sprache:	eng
Schlagworte:	Integrin alphaVbeta3 - antagonists & inhibitors Integrins - antagonists & inhibitors Naphthyridines - chemical synthesis Naphthyridines - chemistry Naphthyridines - pharmacology Quinolines - chemical synthesis Quinolines - chemistry Quinolines - pharmacology Receptors, Vitronectin - antagonists & inhibitors Stereoisomerism X-Ray Diffraction
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