2-甲基-5,6-次甲二氧-3-吲(口朶)丙胺衍生物的合成

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。

Synthesis of some derivatives of 2-methyl-3- (gamma-aminopropyl)-5, 6-methylenedioxyindole (author's transl)

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.