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    Thienylacetic acid derivative
    83.
    发明专利
    Thienylacetic acid derivative 失效
    三烯酸衍生物

    公开(公告)号：JPS5920280A

    公开(公告)日：1984-02-01

    申请号：JP12892782

    申请日：1982-07-26

    申请人： Mitsubishi Petrochem Co Ltd ,  Mitsubishi Yuka Yakuhin Kk

    发明人： TAKEDA MAKOTO ,  TANIYAMA EIJI ,  TSUTSUI MIKIO ,  IWANE HIROSHI ,  SHINODA MAKI ,  KADOWAKI SHIYUUICHIROU ,  MIZOGAMI SUSUMU

    IPC分类号： C07D333/32 ,  A61K31/38 ,  A61K31/381 ,  A61P25/04 ,  A61P29/00 ,  C07D333/34 ,  C07D333/42

    摘要： NEW MATERIAL:A thienylacetic acid derivative shown by the formula I (R
    1 is H, methyl, or ethyl; R
    2 is H, or halogen; R
    3 is O, or S; R
    4 and R
    5 are H, halogen, trifluoromethyl, 1W4C alkyl, 1W4C alkoxy, or 1W4C alkylthio) and its salt and ester.
    EXAMPLE: α-[5-(4-Fluorophenoxy)-2-thienyl]propionic acid.
    USE: Having strong antiphlogistic action and analogesic action, useful as a drung. Having low toxicity and also weak side effects.
    PROCESS: For example, a compound shown by the formula II (A is halogen) is reacted with a compound shown by the formula III (M is alkali metal) to give a compound shown by the formula IV, which is reduced to give an alcohol, the hydroxyl group of the alcohol is halogenated, and replaced with a nitro group. The reaction product is hydrolyzed to give a compound shown by the formula I .
    COPYRIGHT: (C)1984,JPO&Japio

    摘要翻译： 新材料：式I所示的噻吩乙酸衍生物（R 1是H，甲基或乙基; R 2是H或卤素; R 3是O或S; R 4和 R 5是H，卤素，三氟甲基，1-4C烷基，1-4C烷氧基或1-4C烷硫基）及其盐和酯。 实施例：α-[5-（4-氟苯氧基）-2-噻吩基]丙酸。 使用：具有强烈的消炎作用和类比作用，作为一种有益的药物。 毒性低，副作用小。 方法：例如，将式II（A为卤素）所示的化合物与式III所示的化合物（M为碱金属）反应，得到式IV所示的化合物，将其还原成醇 ，醇的羟基被卤化，并被硝基取代。 将反应产物水解，得到式I化合物。

    THIOPHENE COMPOUND AND ITS PREPARATION
    84.
    发明专利
    THIOPHENE COMPOUND AND ITS PREPARATION 失效

    公开(公告)号：JPS56100780A

    公开(公告)日：1981-08-12

    申请号：JP357180

    申请日：1980-01-18

    申请人： NIPPON KAYAKU KK

    发明人： TADA SHIYOUJI

    IPC分类号： C07D333/42

    摘要： NEW MATERIAL:Compounds of formula I (X is H, lower alkyl, carbo-lower- alkoxymethyl). EXAMPLE:2-Amino-3-nitrothiophene. USE:A starting material of dyes and agricultural chemicals. PREPARATION:Nitroacetonitrile and a compound of SHCH2COX (e.g., alpha-mercaptoacetaldehyde) are added to a mixed solvent composed of ethanol and water and the condensation reaction is effected by dropping a basic substance such as triethylamine to obtain a thiophene compound of formula I. Further, the compound is dissolved in pyridine and acetyl chloride or the like is added thereto to effect the acylation of the amino group. Then, the nitration is effected with a mixed acid of nitric and sulfuric acids. Finally, the acyl group is hydrolyzed to give the compound of formula II, too.