3-[p-ω-取代氨基烃氧基)-苯甲酰]-吲哚衍生物的合成

本文根据某些吲哚化合物具有抗生育活性,结合多数非甾体抗生育化合物联有碱性醚链的结构特征,设计并合成了以吲哚为母核的四种类型化合物(Ⅰ_1～7,Ⅱ_1～7,Ⅲ_1～7,Ⅳ₁)22个,并验证了三个熔点与文献报道不符的关键中间体。对小白鼠的初步药理试验表明:所合成的化合物均无抗着床作用;Ⅱ₁,Ⅱ₂,Ⅱ₄和Ⅱ₅有明显的镇痛作用;Ⅲ₂和Ⅲ₃则有较强的抗电休克作用。

Synthesis of 3-(P-(omega-disubstituted aminoalkoxy)-benzoyl)-indole derivatives

According to the fact that some indole compounds have antifertility activity and that the basic ether chain is common to most nonsteroidal antifertility compounds, four types of substituted indole derivatives with such structural feature were designed and synthesized for the purpose of searching potential antifertility agents.Compounds listed in table Ⅱ were prepared by the reaction of p-methoxy benzoic acid chloride with magnesium bromide of indole and substituted indoles, cleavage of the methyl groups, and then condensation with various disubstituted aminoalkyl chloride, or by treating magnesium bromide of indole and substituted indoles directly with p=(ω-disubstituted aminoalkoxy) benzoyl chloride. The melting points of the intermediats (14 a～c) obtained by us were not in agreement with those reported previously in the literature. Their structures were confirmed by different methods.Preliminary pharmacological tests showed that in mice all compounds synthesized did not show any antiimplantation activity; Ⅱ₁, Ⅱ₂, Ⅱ₄ and Ⅱ_s exhibited marked analgesic activity; Ⅲ₁ and Ⅲ₄ showed anticonvulsant effect.