发明名称 5H-THIAZOLO(3,2-A)PYRIMIDINE DERIVATIVE
摘要 PROBLEM TO BE SOLVED: To obtain the subject novel compound that is useful as a therapeutic and preventive agent for cerebral function restriction caused by transplantation, head injury, cardiac arrest, acute and/or chronic neurological disorders as an antagonist of metabotropic glutamate receptor and/or as an agonist. SOLUTION: This compound is represented by formula I (R<1> is H, a lower alkoxy or the like; R<2> is a lower alkyl, a lower alkoxy or the like; R<3> -R<12> are each H, a halogen or the like) or its salt, typically (RS)-2-(2,6- dichlorophenyl)-5-(2-methoxyphenyl)-7-methyl-5H-thiazolo [3,2- a]pyrimidine-6-carboxylic 2-dimethylaminoethyl ester. This compound is prepared by reaction of a compound of formula II withα-bromo-acetaldehyde, when necessary, in addition, converting the compound of formula I to its salt. The intermediate compound of formula II is novel and is prepared, for example, by reaction of 4-metoxybenzaldehyde with acetylacetone and thiourea.
申请公布号 JPH1171380(A) 申请公布日期 1999.03.16
申请号 JP19980199363 申请日期 1998.07.15
申请人 F HOFFMANN LA ROCHE AG 发明人 ADAM GEO;KOLCZEWSKI SABINE;MUTEL VINCENT;WICHMANN JUERGEN;WOLTERING THOMAS JOHANNES
分类号 C07D239/22;A61K31/505;A61K31/519;A61P1/08;A61P9/00;A61P13/02;A61P15/00;A61P25/00;A61P25/04;A61P25/18;A61P25/20;A61P25/24;A61P25/26;A61P25/28;A61P25/30;A61P27/02;A61P43/00;C07D239/00;C07D239/40;C07D277/00;C07D513/04;(IPC1-7):C07D513/04 主分类号 C07D239/22
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