朱耀华, 程树福, 濮家溎, 杨祯祥, 彭司勋. 2-甲基-5,6-次甲二氧-3-吲(口朶)丙胺衍生物的合成J. 药学学报, 1979, 14(12): 720-724.
引用本文: 朱耀华, 程树福, 濮家溎, 杨祯祥, 彭司勋. 2-甲基-5,6-次甲二氧-3-吲(口朶)丙胺衍生物的合成J. 药学学报, 1979, 14(12): 720-724.
Zhu Yaohua, Cheng Shufu, Pu Jiagui, Yang Zhenxiang , Peng Sixun, . SYNTHESIS OF SOME DERIVATIVES OF 2-METHYL-3-(γ-AMINOPROPYL)-5, 6-METHYLENEDIOXYINDOLEJ. Acta Pharmaceutica Sinica, 1979, 14(12): 720-724.
Citation: Zhu Yaohua, Cheng Shufu, Pu Jiagui, Yang Zhenxiang , Peng Sixun, . SYNTHESIS OF SOME DERIVATIVES OF 2-METHYL-3-(γ-AMINOPROPYL)-5, 6-METHYLENEDIOXYINDOLEJ. Acta Pharmaceutica Sinica, 1979, 14(12): 720-724.

2-甲基-5,6-次甲二氧-3-吲(口朶)丙胺衍生物的合成

SYNTHESIS OF SOME DERIVATIVES OF 2-METHYL-3-(γ-AMINOPROPYL)-5, 6-METHYLENEDIOXYINDOLE

  • 摘要: 本文报道以胡椒醛为原料,通过2-甲基-5,6-次甲二氧-3-吲哚丙酸,合成了8个2-甲基-5,6-次甲二氧-3-吲哚丙胺衍生物,药理初步试验,发现化合物(Ⅳ)具有显著增强环已烯巴比妥的作用,且毒性较小。

     

    Abstract: In continuation of our study on indole derivatives, eight substituted 3-(γ-aminopropyl)-indoles were prepared. 2-Methyl-5,6-methylenedioxyindole reacted with acrylic acid in the presence of acetic anhydride to give 2-metbyl-5,6-methylenedioxyindolepro-pionic acid, which on treatment with SiCl4 followed by reaction with requisite amines gave the corresponding amides. The amides thus obtained were readily reduced to the expected products with LiAlH4.An attempt to obtain the title compounds by treating substituted indole with malonyl chloride followed by amination and reduction was unsuccessful.Preliminary pharmacological tests revealed that compound Ⅳ showed marked effect on potentiation of hexobarbital hypnosis with relatively low toxicity.

     

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