Thiazole derivatives useful in therapy as anti-depressant agents
    4.
    发明授权
    Thiazole derivatives useful in therapy as anti-depressant agents 失效
    噻唑衍生物用于治疗作为抗抑郁剂

    公开(公告)号:US4282225A

    公开(公告)日:1981-08-04

    申请号:US117990

    申请日:1980-02-04

    申请人: Dennis C. H. Bigg

    发明人: Dennis C. H. Bigg

    CPC分类号: C07D513/04

    摘要: Thiazole derivatives of general formula (I) ##STR1## in which n is 1 or 2 and Ar represents a phenyl radical unsubstituted or substituted by one or more substituents selected from halogen atoms, the radical CF.sub.3, the phenyl radical straight or branched chain alkyl radicals having 1 to 4 carbon atoms, and cycloalkyl radicals having 3 to 6 carbon atoms, and their pharmaceutically acceptable acid addition salts are useful in therapy as anti-depressive agents. They are prepared by reacting the thiazole ##STR2## with a ketone X--CH.sub.2 --CO--CH.sub.2 O--Ar (III) (X is a leaving group, such as halogen).

    摘要翻译: 通式(I)的噻唑衍生物其中n为1或2,Ar表示未被取代或被一个或多个选自卤素原子,基团CF 3,苯基直链或支链的取代基取代的苯基 具有1至4个碳原子的链烷基和具有3至6个碳原子的环烷基,及其药学上可接受的酸加成盐可用作抗抑郁剂的治疗。 它们通过使噻唑< IMAGE>与酮X-CH 2 -CO-CH 2 O -Ar(III)(X是离去基团,如卤素)反应制备。

    Method of preparing
1-phenyl-1-diethylaminocarbonyl-2-phthalimidomethyl-cyclopropane-z
    5.
    发明授权
    Method of preparing 1-phenyl-1-diethylaminocarbonyl-2-phthalimidomethyl-cyclopropane-z 失效
    1-苯基-1-二乙基氨基羰基-2-邻苯二甲酰亚氨基甲基 - 环丙烷-z的制备方法

    公开(公告)号:US5034541A

    公开(公告)日:1991-07-23

    申请号:US457352

    申请日:1989-12-27

    IPC分类号: C07D209/48 C07D209/49

    CPC分类号: C07D209/48

    摘要: A method of preparing 1-phenyl-1-diethylaminocarbonyl-2-phthalimidomethyl-cyclopropane-Z and key intermediates therefor are disclosed.This method is characterized by the following successive steps:opening of the 1-phenyl-2-oxo-3-oxa-bicyclo(3:1:0)-hexane by diethylamine or a tertiary amine with the aid of a Lewis acid/amine complex:the 1-phenyl-1-diethylaminocarbonyl-2-hydroxymethyl-cyclopropane-Z thus obtained is converted into a 2-chlorinated derivative by the action of a chlorination reagent such as thionyl chloride; andthe 1-phenyl-1-diethylaminocarbonyl-2-chloromethylcyclopropane-Z is reacted with a phthalimide salt in an organic solvent to produce the 1-phenyl-1-diethylaminocarbonyl-2-phthaliumidomethyl-cyclopropane-Z.

    摘要翻译: 公开了制备1-苯基-1-二乙基氨基羰基-2-邻苯二甲酰亚氨基甲基 - 环丙烷-Z的方法及其关键中间体。 该方法的特征在于以下连续步骤:借助路易斯酸/胺,通过二乙胺或叔胺打开1-苯基-2-氧代-3-氧杂双环(3:1:0) - 己烷 络合物:将由此获得的1-苯基-1-二乙基氨基羰基-2-羟甲基 - 环丙烷-Z通过氯化试剂如亚硫酰氯的作用转化为2-氯代衍生物; 并将1-苯基-1-二乙基氨基羰基-2-氯甲基环丙烷-Z与邻苯二甲酰亚胺盐在有机溶剂中反应,生成1-苯基-1-二乙基氨基羰基-2-邻苯二甲酰基甲基 - 环丙烷-Z。