首页> 外国专利> process for the preparation of aliphatic substituted arylchalcogeenkool - waterstofderivaten, methods for the preparation of pharmaceutical preparations.and the re - formed pharmaceutical preparations.

process for the preparation of aliphatic substituted arylchalcogeenkool - waterstofderivaten, methods for the preparation of pharmaceutical preparations.and the re - formed pharmaceutical preparations.

机译:脂族取代的芳基邻苯二甲双胍醇-水硬脂酸酯的制备方法,药物制剂的制备方法和重制的药物制剂。

摘要

Derivs. of formula R1-Ph-X-alk-Y (I) (where R1 is a mono- or bicyclic cycloaliphatic hydrocarbon residue, Ph is opt. substd. phenylene, X is O or S, alk is 1,2-alkenylene, and Y is an opt. functionally modified carboxyl group) (e.g. ethyl p- p-(1-cyclohexenyl)-phenoxy -crotonate) are new compounds which may be prepd. by reacting a cpd. of the formula R1-Ph-XH (II) with a cpd. alk'-Y (III) (where alk' is the 2-Z-1-alkenyl or 1-alkynyl residue corresponding to alk, and Z is an opt. reactively esterified OH group, a 2-hydroxy-1-alkenyl residue opt. being present in the form of the tautomeric 2-oxo-alkyl residue). Prods. of formula (I) obtd. may be converted into different compounds of formula (I). Isomer or racemate mixts. obtd. may be septd. into the individual isomers or racemates, and racemates obtd. may be septd. into the optical antipodes. Salts obtd. may be converted into the corresponding free cpds., or the free cpds. may be converted into their salts. (I) are useful as antiallergic agents (they inhibit histamine release and anaphylactic reactions) and hypolipaemic agents (they lower blood cholesterol and triglyceride levels in rats in standard tests).
机译:派生。式R1-Ph-X-alk-Y(I)的通式(其中R1是单环或双环脂环族烃残基,Ph是亚苯基),X是O或S,alk是1,2-亚链烯基, Y是经优化的功能改性的羧基)(例如对-对-(1-环己烯基)-苯氧基-巴豆酸乙酯)是可以制备的新化合物。通过反应一个cpd。具有cpd的式R1-Ph-XH(II)的通式。 alk'-Y(III)(其中alk'是与alk相对应的2-Z-1-烯基或1-炔基残基,Z是一个反应性酯化的OH基,一个2-羟基-1-烯基残基(以互变异构体2-氧代烷基残基的形式存在)。产品。式(I)的化合物。可以将其转化成不同的式(I)化合物。异构体或外消旋混合物。 t。可能是九月。进入单个的异构体或外消旋体,然后消旋。可能是九月。进入光学对映体。盐类。可以转换为相应的空闲cpds。可能会转化为其盐。 (I)可用作抗过敏药(它们抑制组胺释放和过敏反应)和降血脂药(它们在标准测试中可降低大鼠的血液胆固醇和甘油三酸酯水平)。

著录项

  • 公开/公告号NL7412260A

    专利类型

  • 公开/公告日1975-03-20

    原文格式PDF

  • 申请/专利权人 CIBA-GEIGY A.G. TE BAZEL ZWITSERLAND.;

    申请/专利号NL19740012260

  • 发明设计人

    申请日1974-09-16

  • 分类号C07C59/25;A61K31/19;C07C149/40;

  • 国家 NL

  • 入库时间 2022-08-23 04:36:28

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