Production technique of tenofovir disoproxil fumarate

A technology of tenofovir disoproxil fumarate and tenofovir disoproxil is applied in the field of production technology of tenofovir disoproxil fumarate, and can solve the problems of low yield, low quality, large residual impurities and the like, To achieve the effect of simple post-processing operation, mild reaction conditions and low production cost

Inactive Publication Date: 2016-05-11
JINGMEN SHUAIBANG CHEM SCI & TECHCO
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Problems solved by technology

At present, the traditional method of preparing tenofovir disoproxil fumarate has the disadvantages of large number of impurities and large residues of impurities, low quality, and low yield, which limits further industrial scale-up production

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0016] ①. Add 10kg of tenofovir, 30kg of N-methylpyrrolidone and 11kg of triethylamine into the glass-lined reactor, raise the temperature to 55-59℃, then add 26kg of chloromethyl isopropyl carbonate dropwise, and control the dropping temperature 56-58°C, the dropwise addition time is 1.5-2 hours, after the dropwise addition is completed, continue the heat preservation reaction for 2.5-3.5 hours, and the reaction solution is obtained after the reaction is completed;

[0017] ②. Prepare 600kg of ice-water mixture in a clean reactor, add 50kg of industrial salt to the stirring process and continue stirring to cool down to -10°C, add the reaction liquid obtained in step ① into the ice-water mixture dropwise, stir for 2 hours, and put it in the reactor A large amount of white solids were precipitated. After the ice in the reaction kettle was completely dissolved, the filter cake was rinsed with 60kg of water at 0-5°C, and tenofovir was obtained after drying. The purity of HPLC was ...

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Abstract

The invention provides a production technique of tenofovir disoproxil fumarate. The production technique comprises the following steps: directly adding an ice-water mixture into a reaction solution in the tenofovir disoproxil fumarate preparation process, and crystallizing by physical cooling to obtain the tenofovir disoproxil fumarate, wherein excessive chloromethyl isopropyl carbonate and other organic solvents, the catalyst and impurities can completely enter the water layer; and dissolving in dichloromethane, and washing with water to remove a small amount of impurities entrained by the tenofovir disoproxil fumarate to obtain the tenofovir disoproxil fumarate with the purity of 95% or above, wherein the purity of the product after direct salification is up to 99% or above.

Description

technical field [0001] The invention relates to a production process of tenofovir disoproxil fumarate. Background technique [0002] Tenofovir disoproxil fumarate (chemical name: 9-[(R)-2-[[bis[[(isopropoxycarbonyl)oxy]methoxy]phosphoryl]methoxy]propyl]adeno Purine fumarate), developed by GleadSciences of the United States, was first listed in the United States in October 2001. It is an acyclic nucleoside phosphate compound with anti-HIV and anti-HBV activity, which is tenofovir (II) (chemical name: (R)-9-(2-phosphorylmethoxypropyl) adenine) After entering the human body, the prodrug will be hydrolyzed to release tenofovir and produce antiviral effect. At present, the traditional method of preparing tenofovir disoproxil fumarate has the disadvantages of large number of impurities and large residues of impurities, low quality, and low yield, which limits further industrial scale-up production. Contents of the invention [0003] In order to solve the above problems, the p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6561C07C57/15C07C51/41
CPCC07F9/65616C07C51/412C07C57/15
Inventor 李建华赵协超
Owner JINGMEN SHUAIBANG CHEM SCI & TECHCO
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