冉允章, 吴培金, 文广伶, 张其楷. 抗胆碱能药物的研究 3-取代托品衍生物的合成J. 药学学报, 1984, 19(5): 361-366.
引用本文: 冉允章, 吴培金, 文广伶, 张其楷. 抗胆碱能药物的研究 3-取代托品衍生物的合成J. 药学学报, 1984, 19(5): 361-366.
RAN Yun-zhang, WU Pei-jin, WEN Guang-ling , ZHANG Qi-kai, . STUDIES ON ANTICHOLINERGICS:SYNTHESIS OF 3-SUBSTITUTED TROPANE DERIVATIVESJ. Acta Pharmaceutica Sinica, 1984, 19(5): 361-366.
Citation: RAN Yun-zhang, WU Pei-jin, WEN Guang-ling , ZHANG Qi-kai, . STUDIES ON ANTICHOLINERGICS:SYNTHESIS OF 3-SUBSTITUTED TROPANE DERIVATIVESJ. Acta Pharmaceutica Sinica, 1984, 19(5): 361-366.

抗胆碱能药物的研究 3-取代托品衍生物的合成

STUDIES ON ANTICHOLINERGICS:SYNTHESIS OF 3-SUBSTITUTED TROPANE DERIVATIVES

  • 摘要: 本文报道24个3-取代托品乙醇类、乙烯类和乙烷类化合物的合成。药理筛选结果表明:大多数化合物有明显的抗胆碱能作用,且中枢与外周作用相当。

     

    Abstract: Twenty-four 3-substituted tropanyl ethanols, ethenes and ethanes were synthesized with 3-tropanone as starting material. Through Wittig reaction, hydrogenation and Grignard reaction, 3-substituted tropanylmethyl ketones (Ⅳ1~6) were obtained.By catalytic hydrogenation of ketone Ⅳ1, the corresponding alcohol Ⅴ1 was easily obtained. The ketones Ⅳ2~6 were reacted with corresponding bromides and lithium to form the corresponding alcohols Ⅴ2~6. However, the alcohols (V7~8)could be obtained directly from ethyl (3-tropanyl) acetate, the corresponding bromide and lithium. By dehydration of the alcohols V, the corresponding alkenes VI were formed. The alkenes VI gave the corresponding alkanes VII through catalytic hydrogenation.The anticholinergic action of all these compounds were tested preliminarily in mice and most of them exhibited marked actions. The structure-activity relationship was briefly discussed.

     

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