首页> 外国专利> SYNTHESIS OF DIINDOLYLMETHANES AND INDOLO3,2-BCARBAZOLES, COMPOUNDS FORMED THEREBY, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

SYNTHESIS OF DIINDOLYLMETHANES AND INDOLO3,2-BCARBAZOLES, COMPOUNDS FORMED THEREBY, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

机译:二吲哚甲烷和吲哚[3,2-B]咔唑,由其合成的化合物以及包含它们的药物成分的合成

摘要

Described is a method to make diindolylmethanes and indolyl/pyrrolylmethanes, The method includes the steps of contacting an ether comprising an arylpropargyl moiety and an amine-protected, substituted or unsubstituted aniline moiety with a substituted or unsubstituted indol or a substituted or unsubstituted pyrrole, in the presence of a metal-containing catalyst, for a time and at a temperature to cause an annulation/arylation cascade reaction that yields a diindolylmethane or a indolyl/pyrrolylmethane. The resulting compounds are effective to modulate activity of arylhydrocarbon receptors, to inhibit activity of PCSK9, and to stimulate secretion of glucagon-like peptide 1 in mammals.
机译:描述了一种制备二吲哚基甲烷和吲哚基/吡咯基甲烷的方法,该方法包括以下步骤:使包含芳基炔丙基部分和胺保护的,取代或未取代的苯胺部分的醚与取代或未取代的吲哚或取代或未取代的吡咯接触。在一定时间和温度下在含金属催化剂的存在下引起环化/芳基化级联反应,生成二吲哚基甲烷或吲哚基/吡咯基甲烷。所得化合物可有效地调节芳基烃受体的活性,抑制PCSK9的活性,并刺激哺乳动物体内胰高血糖素样肽1的分泌。

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