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 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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