发明名称 PROCESSES FOR THE PREPARATION OF 4- 4- 4-(2 -CYANOETHENYL)-2,6-DIMETHYLPHENYL )AMINO) -2-PYRIMIDINYL)AMINO BENZONITRILE
摘要 Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).
申请公布号 EP1529032(A1) 申请公布日期 2005.05.11
申请号 EP20030787813 申请日期 2003.08.07
申请人 JANSSEN PHARMACEUTICA NV 发明人 SCHILS, DIDIER P. R.;WILLEMS, JOANNES J. M.;MEDAER, B. P. A. M. J.;PASQUIER, E., T. J.;JANSSEN, PAUL,ADRIAAN,JAN;HEERES, JAN;LEENDERS, RUBEN GERARDUS GEORGE;GUILLEMONT, JEROME, E.G.
分类号 A61K31/505;A61P31/18;C07B61/00;C07C253/20;C07C253/30;C07C255/07;C07C255/42;C07D239/48;(IPC1-7):C07C255/42 主分类号 A61K31/505
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