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2-Ethyl-1H-benzimidazole-6-carboxylic acid synthesis

2synthesis methods
802294-64-0 Synthesis
Propionic-2,3-14C1 acid (8CI)

802294-64-0
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2-Ethyl-1H-benzimidazole-6-carboxylic acid

891454-18-5
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Yield:-

Reaction Conditions:

with hydrogenchloride;formic acid in water;Reflux;

Steps:

General procedure for the preparation of 2-alkylbenzimidazole-5-carboxylic ester (3)

General procedure: To a solution of 3,4-diaminobenzoic acid (0.62g, 4.00 mmol) in concentrated HCl (5mL) was added 88% formic acid (2.00 ml, 24.00 mml). The resulting solution was refluxed for 12-24 h. After the completion of the reaction, the reaction mixture was cooled and neutralized to pH 3-4 with ammonia water. The precipitated product was collected and crystallized from ethanol-water to give 2-alkylbenzimidazole-5-carboxylic acid (2) as solids.

References:

Cong, Chao;Wang, Haiyang;Hu, Yue;Liu, Chen;Ma, Siti;Li, Xin;Cao, Jichao;Ma, Shutao [European Journal of Medicinal Chemistry,2011,vol. 46,# 7,p. 3105 - 3111] Location in patent:supporting information; experimental part