Xie Ning, Li Yanyang, Sun Huifang
2014
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Journal
Chinese Journal of Pharmaceuticals
Abstract
Cabozantinib(S)-malate, an antineoplastic agent, was synthesized from 3,4-dimethoxyaniline(2) by substitution with 5-(methoxymethylene)-2,2-dimethyl-1,3-dioxane-4,6-dione, cyclization, chlorination and nucleophilic substitution with p-nitrophenol to give 6,7-dimethoxy-4-(4-nitrophenoxy)quinoline, which was subjected to Pd/C-H2reduction, acylation and salt forming reaction with an overall yield of about 44%(based on 2).