首页> 外国专利> PROCESS FOR PREPARING ENTACAPONE SUBSTANTIALLY FREE OF Z-ISOMER, SYNTHESIS INTERMEDIATES THEREOF AND A NEW CRYSTALLINE FORM

PROCESS FOR PREPARING ENTACAPONE SUBSTANTIALLY FREE OF Z-ISOMER, SYNTHESIS INTERMEDIATES THEREOF AND A NEW CRYSTALLINE FORM

机译:制备基本不含Z-异构体的对映体的方法,合成过程为其中间体和一种新的结晶形式

摘要

The present invention relates to a new method for obtaining Entacapone substantially free of Z-isomer from 3,4-dihydroxy-5-Nitrobenzaldehyde and N,N-Dimethylcyanoacetamide, or directly from a mixture of (E)- and (Z)-isomers of Entacapone, by formation of organic or inorganic salts, specially piperidine and sodium ones. A new crystalline form G of Entacapone can be obtained from this method in a fast, efficient, and simple way and substantially free of Z-isomer. Another object of the invention is a pharmaceutical composition comprising it.
机译:本发明涉及一种从3,4-二羟基-5-硝基苯甲醛和N,N-二甲基氰基乙酰胺或直接从(E)-和(Z)-异构体的混合物中获得基本上不含Z-异构体的恩他卡朋的新方法通过形成有机盐或无机盐,特别是哌啶和钠盐而制成的恩他卡朋。可以从该方法以快速,有效和简单的方式获得恩他卡朋的新的晶体形式G,并且基本上不含Z-异构体。本发明的另一个目的是包含它的药物组合物。

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