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    Ortho-aminomethylphenol derivative
    64.
    发明专利
    Ortho-aminomethylphenol derivative 失效
    正丙氨基苯酚衍生物

    公开(公告)号：JPS6143153A

    公开(公告)日：1986-03-01

    申请号：JP16446084

    申请日：1984-08-06

    Applicant: Yoshitomi Pharmaceut Ind Ltd

    Inventor： YAMANAKA TSUTOMU ,  YAOKA OSAMU

    IPC: A61K31/15 ,  A61K31/35 ,  A61K31/352 ,  A61K31/47 ,  A61P7/10 ,  A61P9/12 ,  A61P25/04 ,  A61P29/00 ,  C07C67/00 ,  C07C239/00 ,  C07C251/48 ,  C07D215/42 ,  C07D311/68

    CPC classification number: C07D311/68

    Abstract: NEW MATERIAL:A compound shown by the formula I [X is H, or halogen; R is H, or lower alkyl; A is lower alkyl, aryl, aralkyl, or -(CH
    2 )
    n - (n is 2, or e), etc.].
    EXAMPLE: 3'-Aminomethyl-5'-bromo-4'-hydroxypropiophenone oxime.
    USE: A drug having anti-inflammatory, analgestic, diuretic, and hydrotensive actions. Useful for remedying diseases resulting from inflammation, edema, hypertension, etc. Having improved safety.
    PREPARATION: A compound shown by the formula II is reacted with a compound shown by the formula H
    2 N-OR in a inert solvent in the presence of an alkali hydroxide or an organic base, to give a compound shown by the formula I.
    COPYRIGHT: (C)1986,JPO&Japio

    Abstract translation: 新材料：由式I表示的化合物[X是H或卤素; R为H或低级烷基; A是低级烷基，芳基，芳烷基或 - （CH 2）n - （n是2或e）等]。 实施例：3'-氨基甲基-5'-溴-4'-羟基苯丙酮肟。 用途：具有抗炎，止痛，利尿和降压作用的药物。 用于治疗由炎症，水肿，高血压等引起的疾病。有改善的安全性。 制备：将式II化合物与式H2N-OR所示的化合物在惰性溶剂中，在碱金属氢氧化物或有机碱的存在下反应，得到式I所示的化合物。

    NOVEL 4-OXIMINO-1,2,3,4-TETRAHYDROQUINOLINE DERIVATIVE
    65.
    发明专利
    NOVEL 4-OXIMINO-1,2,3,4-TETRAHYDROQUINOLINE DERIVATIVE 失效

    公开(公告)号：JPS57154169A

    公开(公告)日：1982-09-22

    申请号：JP3991181

    申请日：1981-03-19

    Applicant: HODOGAYA CHEMICAL CO LTD ,  MOCHIDA PHARM CO LTD

    Inventor： JINBOU SUSUMU ,  KOUNO SHIYOUICHI ,  KASHIMA KOUICHI

    IPC: C07D215/42 ,  A61K31/47 ,  A61P3/00 ,  A61P7/10 ,  A61P29/00

    Abstract: NEW MATERIAL:The 4-oximino-1,2,3,4-tetrahydroquinoline derivative of formula (R is alkyl; X is F, Cl or Br). EXAMPLE:6-Chloro-4-oximino-1-methoxycarbonyl-1,2,3,4-tetrahydroquinoline. USE:Medicine. It has strong antihydropic and diuretic activities, and extremely low adverse effect to the digestive organs. PROCESS:The compound of formulaIis prepared e.g. by (1) heating a p-halogen- substituted aniline and an acrylic acid ester in a solvent, (2) hydrolyzing the resultant compound and heating in the presence of a dehydrating agent to afford a 6-halogen-substituted 4-oxo-1,2,3,4-tetrahydroquinoline, (3) reacting the compound with various chloroformate which can condense the compound to effect the N-alkoxy-carbonylation of the product, and (4) heating the resultant compound in a mixed solvent of pyridine and alcohol in the presence of hydroxylamine hydrochloride.

    Novel 4-hydroxyimino-1,2,3,4-tetrahydroquinoline derivative
    66.
    发明专利
    Novel 4-hydroxyimino-1,2,3,4-tetrahydroquinoline derivative 失效
    新型4-羟基咪唑-1,2,3,4-四氢喹啉衍生物

    公开(公告)号：JPS5728052A

    公开(公告)日：1982-02-15

    申请号：JP10327280

    申请日：1980-07-28

    Applicant: Hodogaya Chem Co Ltd ,  Mochida Pharmaceut Co Ltd

    Inventor： JINBOU SUSUMU ,  KOUNO SHIYOUICHI ,  KASHIMA KOUICHI

    IPC: C07D215/42 ,  A61K31/47 ,  A61P3/00 ,  A61P7/10 ,  A61P29/00 ,  C07D215/22 ,  C07D401/06

    Abstract: NEW MATERIAL:A 4-hydroxyimino-1,2,3,4-tetrahydroquinoline derivative expressed by the formula (R is H, alkyl, halogen substituted lower alkyl, phenyl substituted lower alkyl, phenylalkenyl, aromatic group containing nitrogen or alkyl or phenyl substituted amino). EXAMPLE:6-Chloro-4-hydroxyimino-1-formyl-1,2,3,4-tetrahydroquinoline. USE:An antihydrophic and a diuretic agent with almost no gastric disorder. PROCESS:p-Chloroaniline is heated with an acrylic ester in a solvent, e.g. benzene, or if desired with a base, e.g. sodium hydride, at room temperature or under heating to carry out the Michael addition reaction to obtain a 3-(p-chlorophenylamino) propionic ester. The resultant ester is hydrolyzed and then heated in the presence of a dehydrating agent to afford the compound expressed by the formula.

    Abstract translation: 新材料：由式（R为H，烷基，卤素取代的低级烷基，苯基取代的低级烷基，苯基烯基，含有氮或烷基的苯基或苯基取代的）表示的4-羟基亚氨基-1,2,3,4-四氢喹啉衍生物 氨基）。 实例：6-氯-4-羟基亚氨基-1-甲酰基-1,2,3,4-四氢喹啉。 用途：具有几乎无胃紊乱的抗肝功能和利尿剂。 方法：将对氯苯胺与丙烯酸酯在溶剂中加热， 苯，或如果需要，用碱，例如 氢化钠，在室温或加热下进行迈克尔加成反应，得到3-（对氯苯基氨基）丙酸酯。 将所得酯水解，然后在脱水剂存在下加热，得到由式表示的化合物。

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