528560-93-2Relevant articles and documents
Preparation method of telmisartan
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Paragraph 0027; 0036-0037; 0040; 0049-0050; 0053; 0062-0063, (2021/08/28)
The invention relates to a preparation method of telmisartan. According to the preparation method, 3-methyl-4-n-butylamide benzoic acid is used as a raw material, an intermediate (1) is prepared through cyaniding, nitration, reduction, ring closing and other reactions, the intermediate (1) and 4 '-bromomethyl biphenyl-2-methyl formate are subjected to condensation to generate an intermediate (2), the intermediate (2) and N-methyl o-phenylenediamine are subjected to condensation to prepare an intermediate (3), and finally the telmisartan is prepared through hydrolysis. The invention develops a new preparation method of telmisartan. The raw material 3-methyl-4-n-butyrylamide benzoic acid adopted by the method is easy to obtain and low in price; the method is mild in reaction condition, easy to operate and high in yield, the cyanation reaction avoids the use of toxic cyanide, the environmental pollution is small, and the method is suitable for industrial production.
MANUFACTURING METHOD OF BIPHENYL-2-CARBOXYLIC ACID METHYL ESTER
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Paragraph 0045-0071, (2019/12/25)
PROBLEM TO BE SOLVED: To provide a manufacturing method of 4'-{[4-methyl-6-(1-methyl-1H-benzimidazole-2-yl)-2-propyl-1H-benzimidazole-1-yl]methyl}biphenyl-2-carboxylic acid methyl ester, capable of improving yield and quality, and enhancing efficiency of workability in an industrial scale. SOLUTION: There is provided a manufacturing method of 4'-{[4-methyl-6-(1-methyl-1H-benzimidazole-2-yl)-2-propyl-1H-benzimidazole-1-yl]methyl}biphenyl-2-carboxylic acid methyl ester by adding water to a reaction mixture containing an organic polar solvent and 4'-{[4-methyl-6-(1-methyl-1H-benzimidazole-2-yl)-2-propyl-1H-benzimidazole-1-yl]methyl}biphenyl-2-carboxylic acid methyl ester generated by mixing a mixture obtained by adding 2-n-propyl-4-methyl-6-(1'-methylbenzimidazole-2-yl)benzimidazole and a base to an organic polar solvent, and 4'-bromomethyl biphenyl-2-carboxylic acid methyl ester, to crystallize the methyl ester. SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
METHOD FOR PRODUCING AMMONIUM SALT OF TELMISARTAN
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Paragraph 0047, (2017/02/23)
PROBLEM TO BE SOLVED: To provide a method for producing an ammonium salt of telmisartan effective as a hypotensive agent with high purity. SOLUTION: The method for producing an ammonium salt of telmisartan comprises a dissolution step of dissolving a crude body of telmisartan by adding, in a mixed solvent of water, a 2-12C alcohol and ethyl acetate, ammonia in an amount of 2.0 to 30.0 mol based on 1 mol of the telmisartan at 0 to 30°C to form an ammonium salt of telmisartan and a crystallization step of depositing the ammonium salt of telmisartan from the solution produced in the dissolution step at 0 to 30°C and achieves reduction of specific impurities C and D. SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT