发明名称 Process for the preparation of optical isomers of thiazolo¬3,2-a pyrimidines, isomers, pharmaceutical compositions containing them and intermediates for this process
摘要 <p>Process for the preparation of optical isomers of products of formula (I) in which R = C6H5 or C6H5CH2 optionally substituted by one or more halogens, alkyl, alkoxy, alkylthio (1-4 C) or else R = alkyl (1-4 C) unsubstituted or substituted by 1 to 3 halogens, alkenyl (2-4 C) or cycloalkyl (3-6 C) and R1 = H or else R and R1, which are different, denote C6H5 or C6H5CH2 optionally substituted by 1 or more halogens, alkyl, alkoxy or alkylthio (1-4 C) or else denote alkyl (1-4 C) consisting in: a) opening the racemic product of formula (I) into racemic product (II), b) reacting the racemic product (II) with an optically active amine to obtain a product (III) in the form of a mixture of two diastereoisomeric forms, c) separating the mixture of the two diastereoisomeric forms of the product of formula (III), d) separately hydrolysing and cyclising each of these forms to obtain the optically active product (I). The invention also relates to the optically active isomers (I) obtained and the intermediates (II) needed for applying the process. &lt;IMAGE&gt;</p>
申请公布号 EP0188150(A1) 申请公布日期 1986.07.23
申请号 EP19850402448 申请日期 1985.12.10
申请人 RHONE-POULENC SANTE 发明人 FABRE, JEAN-LOUIS;FARGE, DANIEL;JAMES, CLAUDE
分类号 A61K31/505;A61P29/00;A61P37/08;C07D277/18;C07D513/04;(IPC1-7):C07D513/04;C07B57/00 主分类号 A61K31/505
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