Zheng Zhi-bing
2008
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Journal
Chinese Journal of Medicinal Chemistry
Abstract
Aim To synthesize novel anti gout drug febuxostat(1).Methods 4-Hydroxybenzonitrile(2) as the starting material was transformed to 4-hydroxy-thiobenzamide(3) via thioformylation.And ethyl 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylate(4),which was synthesized via cyclization from 3,was treated with hexamethylenetetramine to generate the intermediate ethyl 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylate(5).The target compound febuxostat(1) was obtained from 5 by etherification,cyanidation,hydrolysis.Results and conclusion The related structures of intermediates and product were identified by 1H-NMR and FAB-MS.This improved procedure has several advantages of low consumption,mild condition,and convenient operation.