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Losartan preparation method

A technology for the preparation process and compound, applied in the production of bulk chemicals, organic chemistry, etc., can solve the problems of side reactions, affecting the quality of the final product, etc.

Active Publication Date: 2009-02-11
CHINA RESOURCES SAIKE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In our research, we found that if a short-chain alcohol (such as methanol) is used as a reaction solvent, the following side reactions will occur during the reaction, which will affect the quality of the final product

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] 32g 2-butyl-4-chloro-5-hydroxymethyl-1-[2'-(1-trityl-tetrazolyl-5-)biphenyl-4-]methylimidazole, 80ml 2 - dodecyl alcohol, then add 3 g of 20% dilute hydrochloric acid, and stir at room temperature for 24 hours to obtain. The liquid phase tracking spectrum of the finished product is shown in figure 1

[0016] current technology:

[0017] 32g 2-butyl-4-chloro-5-hydroxymethyl-1-[2'-(1-trityl-tetrazolyl-5-)biphenyl-4-]methylimidazole, 80ml Methanol, then add 3g of 20% dilute hydrochloric acid, stir at room temperature for 24 hours, the liquid phase tracking spectrum of the finished product is shown in figure 2

[0018] Synthesis and structure identification of impurities

[0019] 10 g of losartan, 50 ml of DMF, 7.8 g of potassium carbonate, and 1.5 ml of methyl iodide were stirred at room temperature for 24 hours to obtain N-methyl losartan with a yield of 23%.

[0020] 1 HNMR (CDCl3): 0.9(t, 3H), 1.2-1.4(m, 2H), 1.5-1.7(m, 2H), 2.6(t, 2H), 3.3(s, 3H), 4.5(s, 2H) ,...

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Abstract

The invention relates to a preparation method of losartan, which comprises the following steps: triphenylmethyl losartan (structure III) is dissolved in a long chain liquid alcohol over C12, inorganic acid (hydrochloride, sulfate, phosphate) aqueous solution is added as a catalyst and the losartan (structure II) is finally obtained after 24 hours -36 hours of reaction at room temperature. By the improvement of the reaction conditions, no side reaction occurs during the reaction process, thereby ensuring the quality of the final products.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry and relates to a preparation method of losartan, an important intermediate of antihypertensive drug losartan potassium. Background technique [0002] In the preparation process of losartan, the process of obtaining losartan by removing trityl of trityl losartan is a key step, usually the reaction is carried out in a C1-C6 alcohol solvent, and the acid used is Commonly used inorganic acids (hydrochloric acid, sulfuric acid, phosphoric acid.), the representative patent is EP0253310. In our research, we found that if a short-chain alcohol (such as methanol) is used as a reaction solvent, the following side reactions will occur during the reaction, which will affect the quality of the final product [0003] [0004] We have found through experiments that using liquid long-chain alcohol as a reaction solvent can effectively solve this problem and achieve the purpose of improving product quality. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/10
CPCY02P20/55
Inventor 闫起强祁伟李志强杨琰王文峰
Owner CHINA RESOURCES SAIKE PHARMA
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