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A process for the preparation of chirally pure N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine

机译：制备手性纯的N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸的方法

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摘要

The present invention relates to a process for the preparation of chirally pure N-(trans-4-isopropyleyelohexylcarbonyl)-D-phenylalanine (nateglinide) of the formula (I)by treating a compound of the general formula (II)wherein R is a lower (C₁-C₄) alkyl group or hydrogen, with a base to yield an alkali salt, and liberating the product from said salt with a mineral acid, characterized in that the acidic liberation of the product is accomplished by adding the acid in two portions in such a way that the first time a less than equimolar amount of the acid is added to yield a mixture of nateglinide and an alkali salt thereof, said mixture is isolated and a further amount of mineral acid is added to the mixture.

机译：本发明涉及一种制备式（I）的手性纯N-（反式-4-异丙基邻苯二甲酰基羰基）-D-苯丙氨酸（那格列奈）的方法 <图像文件=“ IMGA0001.GIF” he =“ 53” id =“ ia01” imgContent =“ chem” imgFormat =“ GIF” wi =“ 66” /> 通过处理通式（II）的化合物 <图像文件=“ IMGA0002.GIF” he =“ 48” id =“ ia02” imgContent =“ chem” imgFormat =“ GIF” wi =“ 57” /> 其中R是具有碱的低级（C _{1 -C _{4 ）烷基或氢，产生碱金属盐，并用矿物从所述盐中释放产物表征为的酸，是通过分两部分添加酸的方式来实现产物的酸释放，这种方式是，第一次添加小于等摩尔量的酸以生成那格列奈及其碱金属盐，将所述混合物分离，并将另外量的无机酸加入到混合物中。}} 展开▼

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公开/公告号EP2264002A1

专利类型

公开/公告日2010-12-22

原文格式PDF

申请/专利权人 RICHTER GEDEON NYRT;
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申请/专利号EP20100181081

发明设计人 HEGEDÛS BÉLA;GIZUR TIBOR;SZEMZÔ ATTILA;TÁRKÁNYI GÁBOR;GAZDAG MÁRIA;BABJÁK MÓNIKA;TÖRLEY JÓZSEF;
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申请日2004-07-08

分类号C07C231/12;C07C231/24;C07C233/63;

国家 EP

入库时间 2022-08-21 17:56:17

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