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    • 94. 发明授权
    • N-Cyclopropylisoindolines
    • N-环丙基异吲哚啉
    • US4351842A
    • 1982-09-28
    • US170929
    • 1980-07-21
    • Richard J. Coles
    • Richard J. Coles
    • C07D209/46A61K31/40A61K31/403A61K31/4035A61P25/26C07C51/367C07C51/373C07D209/44C07D209/48C07D209/58C07D209/60C07D209/62C07D491/04C07D491/056
    • C07D209/48C07C51/367C07C51/373C07D209/44C07D209/58C07D209/60C07D209/62C07D491/04
    • Compounds of the general formula: ##STR1## in which A is a benzene ring or a carbocyclic aromatic group consisting of two or three fused benzene rings, the group A being linked to the nitrogen containing ring at two adjacent carbon atoms and the benzene ring or each benzene ring optionally carrying one or more substituents which may be the same or different, and may be alkyl, aryl, halo, hydroxy, acyloxy or alkoxy, or two adjacent positions in a ring may be substituted so as to form a methylene dioxy group (--O--CH.sub.2 --O--);R.sub.1 and R.sub.2 which may be the same or different, each represent hydrogen; an alkyl group which contains 1 to 6 carbon atoms and which may be substituted; a hydroxycarbonyl or an alkoxycarbonyl group; andone of R.sub.3 and R.sub.4 represents hydrogen, an alkyl group which contains 1 to 6 carbon atoms and which may be substituted, or a hydroxy, alkoxy, hydroxycarbonyl or alkoxycarbonyl group and the other of R.sub.3 and R.sub.4 represents hydrogen, or a non-toxic physiologically acceptable salt or bioprecursor thereof.These compounds are useful in the treatment of patients suffering from depression.
    • 其中A是由两个或三个稠合苯环组成的苯环或碳环芳基,通式为:其中A与两个相邻碳原子上的含氮环连接,苯环或 每个苯环任选地带有一个或多个可以相同或不同的取代基,并且可以是环中的烷基,芳基,卤素,羟基,酰氧基或烷氧基或两个相邻位置,以便形成亚甲基二氧基 (-O-CH 2 -O-); 可以相同或不同的R 1和R 2各自表示氢; 含有1至6个碳原子并可被取代的烷基; 羟基羰基或烷氧基羰基; R 3和R 4中的一个表示氢,可以被取代的碳原子数1〜6的烷基,羟基,烷氧基,羟基羰基或烷氧基羰基,R3和R4中的另一个表示氢,或无毒的 生理上可接受的盐或其生物前体。 这些化合物可用于治疗患有抑郁症的患者。
    • 95. 发明授权
    • Process of preparation of racemic hydroxyarylglycolic acids and novel
products resulting therefrom
    • 制备外消旋羟基芳基乙醇酸及其产生的新产品的方法
    • US4339602A
    • 1982-07-13
    • US243965
    • 1981-02-25
    • Alain SchouteetenYani Christidis
    • Alain SchouteetenYani Christidis
    • C07C59/46C07C51/00C07C51/367C07C59/48C07C65/11C07C59/50
    • C07C51/367
    • The invention relates to a process of preparation of racemic hydroxyarylglycolic acids and the novel products resulting therefrom.According to such process glyoxylic acid is condensed in water in the presence of an alkaline agent at a temperature of between 35.degree. and 100.degree. C., on an excess, or not, of phenolic aromative derivative other than phenol, having at least one proton on either of the ortho or para positions with respect to the phenol function.Application to the production of novel acids such as 4-hydroxy 3-tertiobutyl mandelic acid, 2-hydroxy 5-tertiobutyl mandelic acid, 3-chloro 4-hydroxy mandelic acid, 2-fluoro 4-hydroxy mandelic acid, monohydrated 3,5-dimethoxy 4-hydroxy mandelic acid, 2-hydroxy 5-methyl mandelic acid, (1-hydroxy 2-naphthyl) glycolic acid, 4-ethyl 2-hydroxy mandelic acid, and 4-hydroxy 3-methyl mandelic acid.
    • PCT No.PCT / FR80 / 00126 Sec。 371日期:1981年2月25日 102(e)日期1981年2月25日PCT提交1980年7月24日PCT公布。 公开号WO81 / 00254 日本2月5日,1981年。本发明涉及外消旋羟基芳基乙醇酸的制备方法和由此产生的新产物。 根据这种方法,乙醛酸在碱性试剂存在下,在35℃至100℃的温度下,在除苯酚以外的酚类芳族衍生物的过量或不存在下,在水中冷凝,其具有至少一个质子 在相对于酚官能团的邻位或对位。 适用于生产新型酸如4-羟基-3-叔丁基扁桃酸,2-羟基5-叔丁基扁桃酸,3-氯-4-羟基扁桃酸,2-氟4-羟基扁桃酸,一水合3,5-二 二羟甲基4-羟基扁桃酸,2-羟基-5-甲基扁桃酸,(1-羟基2-萘基)乙醇酸,4-乙基2-羟基扁桃酸和4-羟基3-甲基扁桃酸。