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Process for the preparation of Zafirlukast and analogs thereof

机译:扎鲁司特及其类似物的制备方法

摘要

The present invention relates to a process for the preparation of (1-alkylindol-3-ylmethyl) benzoic acid derivatives, in particular Zafirlukast and analogs thereof. Further, this process is based on protection group free and C—H bond activation strategy involving all step catalytic transformation sequence and comprises the following steps: Sonogashira coupling, indole formation by Sp3 C—H activation, reductive hydrogenation and amidation.
机译:本发明涉及一种制备(1-烷基吲哚-3-基甲基)苯甲酸衍生物,特别是扎鲁司特及其类似物的方法。此外,该过程基于涉及所有步骤催化转化序列的无保护基团和CH键活化策略,并且包括以下步骤:Sonogashira偶联,Sp 3 CHH活化形成吲哚,还原氢化和酰胺化。

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