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Valsartan methyl ester alkali metal salt and preparation method thereof
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A technology of valsartan methyl ester and alkali metal salt, which is applied in the field of valsartan methyl ester alkali metal salt and its preparation, can solve the problems of low optical purity and low chemical purity of valsartan methyl ester, and achieve easy separation Effect
Active Publication Date: 2013-04-03
NANTONG SHIMEIKANG PHARMA CHEM
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[0009] The technical problem to be solved by this invention is to provide a kind of valsartan methyl ester alkali metal salt, in order to solve the problem that the valsartan methyl ester produced by existing technology has low chemical purity and low optical purity
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Embodiment 1
[0026] Embodiment 1: Preparation of valsartan methyl ester sodium salt.
[0027] Add 1000g valsartan methyl ester toluene solution (cyclization reaction solution, containing 22% valsartan methyl ester) in a 3000ml four-neck flask, then add a solution made of 60g sodiumbicarbonate and 540g water, stir at room temperature to form a salt 4 hours, filtered, washed with 100g of toluene, and then washed with 100g of water, and dried in vacuum at 80°C to constant weight to obtain 220g of white valsartan methyl ester sodium salt.
[0032] Embodiment 2: Preparation of valsartan methyl ester potassium salt.
[0033] Add 1000g valsartan methyl acetateethyl acetate solution (containing 25% valsartan methyl ester) to a 3000ml four-necked flask, then add a solution made of 80g sodium bicarbonate and 600g water, stir at room temperature to form a salt for 6 hours, filter , washed with 100g of toluene, then washed with 100g of water, and dried in vacuum at 80°C to constant weight to obtain 260g of white potassium salt of valsartan methyl ester.
[0034] As detected by HPLC, the chemical purity is 99.5%.
[0035] Chiral HPLC detection, the optical purity is 99.1%.
[0036] 1 In HNMR analysis, there was no peak corresponding to the proton on the tetrazole ring.
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Abstract
The invention discloses a valsartan methyl ester alkali metal salt of which the structural formula is as follows. The invention also discloses a preparation method of the valsartan methyl ester alkali metal salt. By using salification and purification, the chemical purity and optical purity of the valsartan methyl ester alkali metal salt are obviously enhanced as compared with the valsartan methyl ester alkali metal salt before salification.
Description
technical field [0001] The invention relates to a valsartan methyl ester alkali metal salt and a preparation method thereof, belonging to the technical field of medicinal chemistry. Background technique [0002] Valsartan methyl ester is the key intermediate for the preparation of the antihypertensive drugValsartan. The Chinese name is: N-(1-pentanoyl)-N-[4-[2-(1H-tetrazolium- 5-base) phenyl] benzyl] -L-valine methyl ester, the structural formula is as follows: [0003] [0004] U.S. Patent US5399578A discloses the preparation method of valsartan methyl ester and valsartan bulk drug: N-(1-pentanoyl)-N-[4-[2-(5-cyano)phenyl]benzyl]- L-valine methyl ester and sodiumazide undergo a cyclization reaction with the participation of an organotin compound to obtain valsartan methyl ester, which is directly hydrolyzed to produce valsartan bulk drug without purification. [0005] [0006] This method uses highly toxic organotin compounds to participate in the cyclization reac...
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