首页> 外国专利> NOVEL OXYACETIC ACID DERIVATIVE, ITS PREPARATION, AND BLOOD LIPID LEVEL DEPRESSING AGENT CONTAINING SAID DERIVATIVE AS ACTIVE COMPONENT

NOVEL OXYACETIC ACID DERIVATIVE, ITS PREPARATION, AND BLOOD LIPID LEVEL DEPRESSING AGENT CONTAINING SAID DERIVATIVE AS ACTIVE COMPONENT

机译:包含所述衍生物的新型氧代乙酸衍生物,其制备和血脂降低剂

摘要

NEW MATERIAL:The oxyacetic acid derivative of formulaI(R1 is H or acyl; R2 is H or lower alkyl). EXAMPLE:alpha-[4-(1-Naphthoylaminoethyl)-phenoxy]-alpha-cyclohexylacetic acid ethyl ester. USE:It has blood lipid level depressing activity, and is useful as a blood lipid depressant for the remedy of hyperlipemia. It has also antithrombogenetic and antiphlogistic activities and low toxicity, and is free from the side effects against the hepatic function. PROCESS:The compound of formulaIcan be prepared by reacting the hydroxyl compound of formula II (R3 is R1-NH or group of formula III) with the alpha- halogeno-cyclohexylacetic acid ethyl ester of formula IV (X is halogen atom; R4 is lower alkyl) in the presence of a solvent such as dimethylformamide, and if necessary, hydrolyzing the product. The molar ratio of the compound of formula II to the compound of formula IV is usually 1:1; however, it is preferable to use one of the compounds in excess.
机译:新材料:式I的氧乙酸衍生物(R 1为H或酰基; R 2为H或低级烷基)。实施例:α-[4-(1-萘甲氨基乙基)-苯氧基]-α-环己基乙酸乙酯。用途:具有降低血脂水平的活性,可作为降血脂药治疗高脂血症。它还具有抗血栓形成和消炎活性,并且毒性低,并且没有针对肝功能的副作用。方法:可以通过使式II的羟基化合物(R 3为R 1 -NH或式III的基团)与式IV的α-卤代-环己基乙酸乙酯反应来制备式I的化合物。卤原子; R 4是低级烷基)在溶剂例如二甲基甲酰胺的存在下,并且如果需要,水解产物。式II化合物与式IV化合物的摩尔比通常为1:1;然而,优选过量使用一种化合物。

著录项

  • 公开/公告号JPH0237344B2

    专利类型

  • 公开/公告日1990-08-23

    原文格式PDF

  • 申请/专利权人 KAKEN PHARMA CO LTD;

    申请/专利号JP19810057072

  • 申请日1981-04-17

  • 分类号A61K31/135;A61K31/16;A61K31/195;A61K31/215;A61K31/34;A61K31/341;A61K31/357;A61K31/38;A61K31/381;A61K31/40;A61P3/06;C07C217/60;C07C233/18;C07C233/60;C07C233/73;C07C235/26;C07C311/17;C07D213/81;C07D307/68;C07D317/68;C07D333/38;

  • 国家 JP

  • 入库时间 2022-08-22 06:20:59

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