PROCESS FOR THE PREPARATION OF ZAFIRLUKAST AND ANALOGS THEREOF

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.