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    • 52. 发明授权
    • 6-(3-diloweralkylamino-propyl)-7-(12h)-pleiadenones and salts thereof
    • 6-(3-二甲基氨基丙基)-7-(12H) - 哌啶酮及其盐
    • US3681461A
    • 1972-08-01
    • US3681461D
    • 1970-08-12
    • SMITH KLINE FRENCH LAB
    • KAISER CARLZIRKLE CHARLES L
    • C07C63/36C07D207/04C07D207/06C07D211/10C07D211/22C07D211/32C07C87/28
    • C07D211/32C07C63/36C07D207/04C07D207/06C07D211/10C07D211/22
    • 7,12-Dihydropleiadenes in which the nucleus may have chloro, methyl, methoxy, methylthio or trifluoromethyl substituents and the 7-position is substituted by an aminopropylidene, aminopropyl, piperidylidene, piperidyl, pyrrolidylidene, pyrrolidyl, 2-piperidinylethylidene, 2-piperidinylethyl, 2pyrrolidinylethylidene or 2-pyrrolidinylethyl moiety are useful as tranquilizers and antidepressants. The compounds are generally prepared by reaction of the appropriate amino Grignard reagent with a 7(12H)-pleiadenone followed by acid dehydration of the 7hydroxy intermediate and subsequent reduction of the unsaturated derivative with phosphorus and hydroiodic acid. The 1,4-addition products also obtained via the Grignard reaction, namely 6substituted-7(12H)-pleiadenones, are also useful as tranquilizers and antidepressants.
    • 7,12-二氢扁桃酸,其中核可以具有氯,甲基,甲氧基,甲硫基或三氟甲基取代基,并且7-位被氨基亚丙基,氨基丙基,哌啶基,哌啶基,吡咯烷亚基,吡咯烷基,2-哌啶子基亚乙基,2-哌啶基乙基, 2-吡咯烷基亚乙基或2-吡咯烷基乙基部分可用作镇定剂和抗抑郁药。 这些化合物通常通过合适的氨基格氏试剂与7(12H) - ι-腺嘌呤反应,然后酸性脱水7-羟基中间体,随后用磷酸和氢碘酸还原不饱和衍生物来制备。 还通过格利雅反应得到的1,4-加成产物,即6-取代-7(12H) - ple酮,也可用作镇定剂和抗抑郁剂。