首页> 外国专利> New procedure for Synthesis of (2S, 3aS, 7aS) perhydroindole-2-carboxylic acid and its esters and their use in the synthesis of perindopril.

New procedure for Synthesis of (2S, 3aS, 7aS) perhydroindole-2-carboxylic acid and its esters and their use in the synthesis of perindopril.

机译:(2S,3aS,7aS)全氢吲哚-2-羧酸及其酯的合成新方法及其在培哚普利的合成中的应用。

摘要

Method for synthesizing compounds of formula ** ** in which R represents a hydrogen atom or a benzyl group or alkyl of 1 to 6 linear or branched carbon, and their addition salts with an acid or an inorganic base or organic. wherein the acid (2- oxocyclohexyl) acetic acid of formula which is condensed with (S) -phenylglycinol, in which Ph represents phenyl group, to yield the tricyclic lactam, in the form of a single diastereoisomer, in which Ph represents the phenyl group, which is reacted with a reducing agent in the presence of a Lewis acid, to yield a compound in which Ph represents the phenyl group, which function 2-hydroxy-1-phenylethyl is separated, that reacts either with triflic anhydride, or with an alkylating reagent.
机译:合成其中R代表氢原子或1-6个直链或支链碳的苄基或烷基的式****化合物的方法,及其与酸或无机碱或有机物的加成盐。其中式(2)的酸(2-氧代环己基)乙酸与(S)-苯基甘醇(其中Ph代表苯基)缩合而得到三环内酰胺,其为单一非对映异构体形式,其中Ph代表苯基在路易斯酸的存在下与还原剂反应,生成一种化合物,其中Ph代表苯基,该官能团的2-羟基-1-苯乙基被分离,该化合物与三氟甲磺酸酐或与三氟甲磺酸酐反应。烷基化试剂。

著录项

  • 公开/公告号ES2233914T3

    专利类型

  • 公开/公告日2005-06-16

    原文格式PDF

  • 申请/专利权人 LES LABORATOIRES SERVIER;

    申请/专利号ES20030291157T

  • 发明设计人 DUBUFFET THIERRY;LECOUVE JEAN-PIERRE;

    申请日2003-05-19

  • 分类号C07D209/42;C07K5/02;C07K5/06;

  • 国家 ES

  • 入库时间 2022-08-21 22:14:41

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