首页> 外国专利> ESTERES SYNTHESIS PROCEDURE OF N - ((S) -1-CARBOXIBUTE) - (S) -ALANINE AND ITS APPLICATION IN PERINDOPRILE SYNTHESIS.

ESTERES SYNTHESIS PROCEDURE OF N - ((S) -1-CARBOXIBUTE) - (S) -ALANINE AND ITS APPLICATION IN PERINDOPRILE SYNTHESIS.

机译:N-((S)-1-CARBOXIBUTE)-(S)-Alanine的酯合成方法及其在吲哚合成中的应用。

摘要

Industrial synthesis process of the compounds of formula (I) where R represents a linear or branched (C1-C6) alkyl group, characterized in that the alanine is condensed, of formula (III): with a compound of formula (IV): where R has the same meaning as in formula (I), under hydrogenation catalyzed by 5% carbon / palladium, in water, under a pressure between 1 and 30 bar, at a temperature between 10 and 60 ° C, in the presence of a amount of sodium hydroxide comprised between 0.5 and 0.5 moles per mole of derivative of formula (IV) used, to drive, after acidification of the reaction medium at a pH between 3 and 3.5, filtration and recrystallization of the precipitate obtained in acetonitrile, to the derivative of optically pure formula (I).
机译:式(I)的化合物的工业合成方法,其中R代表直链或支链(C1-C6)烷基,其特征在于式(III)的丙氨酸是稠合的:与式(IV)的化合物: R具有与式(I)相同的含义,在一定量的存在下,在水中由5%碳/钯催化,在1-30bar的压力下,在10-60℃的温度下,进行氢化。每摩尔所用的式(IV)的衍生物包含0.5至0.5摩尔的氢氧化钠,以在pH 3至3.5之间酸化反应介质后,驱动并过滤乙腈中得到的沉淀物的过滤和重结晶。光学纯的式(I)的化合物。

著录项

  • 公开/公告号ES2287114T3

    专利类型

  • 公开/公告日2007-12-16

    原文格式PDF

  • 申请/专利权人 LES LABORATOIRES SERVIER;

    申请/专利号ES20010923776T

  • 发明设计人 SOUVIE JEAN-CLAUDE;RENAUD ALAIN;

    申请日2001-04-10

  • 分类号A61K38/55;C07C227/32;A61P9;A61P9/04;A61P9/12;A61P43;C07B61;C07C227/42;C07C229/16;C07C229/24;

  • 国家 ES

  • 入库时间 2022-08-21 20:04:29

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