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    3-propionylsalicylic acid derivative and preparation thereof
    6.
    发明专利
    3-propionylsalicylic acid derivative and preparation thereof 失效
    3-丙炔二酸衍生物及其制备方法

    公开(公告)号：JPS5967242A

    公开(公告)日：1984-04-16

    申请号：JP17130482

    申请日：1982-09-30

    申请人： Oosakashi ,  Yamamoto Kagaku Kogyo Kk

    发明人： INOUE HIROSHIGE ,  FUKUSHIMA KENICHI ,  NISHIGUCHI IKUZOU

    IPC分类号： C07C67/00 ,  C07C51/00 ,  C07C51/353 ,  C07C51/373 ,  C07C65/40 ,  C07C69/84 ,  C07C69/88 ,  C07C213/00 ,  C07C219/12 ,  C07D205/08 ,  C07D295/08 ,  C07D295/088 ,  C07D311/30

    CPC分类号： C07D295/088 ,  C07C51/373 ,  C07C65/40 ,  C07D311/30 ,  Y10S514/869 ,  Y10S514/929

    摘要： NEW MATERIAL:A 3-propionylsalicyclic acid derivative of formula I [R is H, lower alkyl or formula II (R
    1 and R
    2 are lower alkyl or R
    1 and R
    2 together with the nitrogen atom to which they are linked through or not through a hetero atom may form a heterocyclic ring; n is an integer 1W4); X is H or halogen, provided that R represents formula II when X is H atom].
    EXAMPLE: Ethyl-5-chloro-3-propionylsalicylate.
    USE: Useful as a remedy for preventing the fit of angina pectoris and cardiac infraction, etc. and a remedy for increasing the discharge capacity of the urinary bladder, disappearance of subjective symptom of thamuria, etc. having coronary arterial vasodilator action and coronary blood stream increasing action, and further useful as a synthetic intermediate for compounds useful as a diuretic having the remissive action, e.g. smooth muscle spasm in the lower urinary tract.
    PROCESS: A compound of formula III (X' is halogen) is reacted with a propionyl halide by the Friedel-Crafts reaction to give the aimed compound of formula I .
    COPYRIGHT: (C)1984,JPO&Japio

    摘要翻译： 新材料：式I的3-丙酰基水杨酸衍生物[R是H，低级烷基或式II（R 1和R 2）是低级烷基或R 1和R 2与氮原子一起 它们通过或不与杂原子连接在一起可以形成杂环; n是整数1-4）; X是H或卤素，条件是当X是H原子时，R表示式II）。 实施例：乙基-5-氯-3- propionylsalicylate。 用途：可用作预防心绞痛和心脏梗死等适应症的补救措施，以及增加膀胱排出能力的补救措施，具有冠状动脉血管扩张作用和冠状动脉血流的饱腹感主要症状消失 增加作用，并且还可用作用作具有缓和作用的利尿剂的化合物的合成中间体，例如 下尿路平滑肌痉挛。 方法：通过Friedel-Crafts反应将式III化合物（X'是卤素）与丙酰卤反应，得到目标化合物I。

    Nitrogen-containing polycyclic compound and its preparation
    9.
    发明专利
    Nitrogen-containing polycyclic compound and its preparation 失效
    含氮的多环化合物及其制备

    公开(公告)号：JPS5732281A

    公开(公告)日：1982-02-20

    申请号：JP10849580

    申请日：1980-08-06

    申请人： Sumitomo Chem Co Ltd

    发明人： ONO KEIICHI ,  KAWAKAMI HAJIME ,  KATSUBE SUMIMOTO

    IPC分类号： A61K31/435 ,  A61K31/44 ,  A61P9/08 ,  A61P25/28 ,  C07D461/00

    CPC分类号： C07D461/00 ,  Y10S514/824 ,  Y10S514/879 ,  Y10S514/929

    摘要： NEW MATERIAL:The nitrogen-containing polycyclic compound of formula I (R
    1 is lower alkyl; R
    2 is aryl) and its salt.
    EXAMPLE: 16-Benzylidene-17-oxo-eburnane.
    USE: Vasodilator, antispasmodic agent and cerebral metabolism activating agent useful as a remedy for arteriosclerosis caused by thrombosis, etc. and cerebral and coronary vessel disorder.
    PROCESS: The compound of formula I is prepared by reacting the ketone derivative of formula II with the aldehyde derivative of formula R
    2 -CHO in a proper solvent (e.g. alcoholic solvent, hydrated alcohol solvent, amide solvent, ether solvent, or aromatic hydrocarbon) in the presence of a base (e.g. metal hydride such as sodium hydride, caustic alkali, alkali metal carbonate, triethylamine, etc.).
    COPYRIGHT: (C)1982,JPO&Japio

    摘要翻译： 新材料：式I的含氮多环化合物（R 1是低级烷基; R 2是芳基）及其盐。 实施例：16-亚苄基-17-氧代 - 伊本烷。 用途：血管扩张剂，抗痉挛剂和脑代谢活化剂，可用作血栓形成引起的动脉硬化症，脑血管疾病和冠状动脉疾病。 方法：式I化合物通过使式II的酮衍生物与式R 2 -CHO的醛衍生物在合适的溶剂（例如醇溶剂，水合醇溶剂，酰胺溶剂，醚溶剂或芳族化合物）中反应来制备 碳氢化合物）在碱（例如金属氢化物如氢化钠，苛性碱，碱金属碳酸盐，三乙胺等）存在下反应。