首页> 外国专利> Crystallization process of 1-2-(naphth-2-yl)ethyl-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride, mixture of form I and form III of 1-2-(naphth-2-yl)ethyl-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride

Crystallization process of 1-2-(naphth-2-yl)ethyl-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride, mixture of form I and form III of 1-2-(naphth-2-yl)ethyl-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride

机译：1- [2-（萘-2-基）乙基] -4-（3-三氟甲基苯基）-1,2,3,6-四氢吡啶盐酸盐，1- [2-的I型和III型混合物（萘-2-基）乙基] -4-（3-三氟甲基苯基）-1,2,3,6-四氢吡啶盐酸盐

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摘要

In the present invention, there is disclosed a crystallization process of 1-[2-(naphth-2-yl)ethyl]-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride comprising the following steps: (a) refluxing of 1-[2-(naphth-2-yl)ethyl]-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride in an ethanol/water mixture in a ratio ranging from 95/5 to 70/30; (b) cooling the resulting product to a temperature in the range of -10 to +10 degC by making use of temperature gradient of 5 to 30 degC per one hour and stirring speed within 0 to 600 rpm; and (c) isolating a mixture of the form I/form III of 1-[2-(naphth-2-yl)ethyl]-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride, in which the ration of the components ranges within 80/20 do 60/40, and optionally reducing particle size of this mixture below 50 microns. Disclosed are also the mixture of form I and form III of the 1-[2-(naphth-2-yl)ethyl]-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride as well as a pharmaceutical composition containing this compound in the form of a crystalline mixture of the form I/form III.

机译：在本发明中，公开了1- [2-（萘-2-基）乙基] -4-（3-三氟甲基苯基）-1，2，3，6-四氢吡啶盐酸盐的结晶方法，该方法包括以下步骤：（a）将1- [2-（萘-2-基）乙基] -4-（3-三氟甲基苯基）-1,2,3,6-四氢吡啶盐酸盐在乙醇/水混合物中回流的比率为95 / 5至70/30; （b）通过使用每1小时5至30℃的温度梯度和0至600rpm的搅拌速度将所得产物冷却至-10至+ 10℃的温度; （c）分离1- [2-（萘-2-基）乙基] -4-（3-三氟甲基苯基）-1，2，3，6-四氢吡啶盐酸盐的形式I /形式III的混合物，成分的比例在80/20至60/40之间，并且可以选择将该混合物的粒径减小到50微米以下。还公开了1- [2-（萘-2-基）乙基] -4-（3-三氟甲基苯基）-1，2，3，6-四氢吡啶盐酸盐的形式I和形式III的混合物，以及药物组合物，其含有形式为I /形式III的结晶混合物形式的该化合物。

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公开/公告号CZ296689B6

专利类型
公开/公告日2006-05-17

原文格式PDF
申请/专利权人 SANOFI-AVENTIS;
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申请/专利号CZ19990002292
发明设计人 CARON ANTOINE;FRANC BRUNO;MONNIER OLIVIER;
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申请日1997-12-23
分类号C07D211/70;A61K31/44;A61K31/445;
国家 CZ
入库时间 2022-08-21 21:39:51

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