Tetrahedron

A novel and practical synthesis of substituted 2-ethoxy benzimidazole: candesartan cilexetil

P Wang, G Zheng, Y Wang, X Wang, Y Li, W Xiang

Index: Wang, Ping; Zheng, Guo-Jun; Wang, Ya-Ping; Wang, Xiang-Jing; Li, Yan; Xiang, Wen-Sheng Tetrahedron, 2010 , vol. 66, # 29 p. 5402 - 5406

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Citation Number: 17

Abstract

A novel and practical synthetic route for the preparation of candesartan cilexetil from methyl 2-amino-3-nitrobenzoate is described. The key steps are the reaction of methyl 2-bromo-3-( diethoxymethyleneamino) benzoate with (2′-(1-trityl-1H-tetrazol-5-yl) biphenyl-4-yl) methanamine and the final formation of 2-ethoxy benzimidazole ring via intramolecular N- arylation. The final ring closure process could be utilized to prepare other 2-substituted ...

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