A novel and practical synthesis of substituted 2-ethoxy benzimidazole: candesartan cilexetil |
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Authors: | Ping Wang Ya-ping Wang Yan Li |
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Institution: | a Department of Biochemical Engineering, Northeast Agricultural University, Harbin 150030, China b Zhejiang Hisun Pharmaceutical Co., Ltd., Taizhou 318000, China |
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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 benzimidazoles. The method is simple for operation and suitable for industrial production. |
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Keywords: | Candesartan cilexetil Receptor antagonist Antihypertensive Synthesis |
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