Method for preparing darunavir

A technology of darunavir and ferric nitrite, applied in organic chemistry and other directions, can solve the problems of high price of darunavir, high requirements for preparation environment, and patients cannot afford the price.

Pending Publication Date: 2020-01-17
ABA CHEM CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Aiming at the deficiencies of the prior art, the present invention provides a preparation method of darunavir, which has the advantages of low preparation cost, and solves the problem that the preparation route of darunavir has been disclosed for a long time, but in the disclosed route method, darunavir The preparation efficiency of navir is low, the preparation cost is high, and the requirements for the preparation environment are also high, resulting in the high price of darunavir finally prepared, and the problem that patients cannot afford such a high price

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment one: a kind of preparation method of darunavir comprises the following steps:

[0022] 1) Take 20 parts of cobalt, 10 parts of triethylamine, 10 parts of ferrous oxide, 10 parts of zinc oxide, 3 parts of 1.2 equivalents of hydrogen methane, 20 parts of zinc, 50 parts of ferric nitrite solution, 30 parts of metal alkali, and 40 parts of aluminum, 10 parts of silicon dioxide, 3 parts of p-acetamidobenzoyl sulfonyl chloride, 3 parts of precipitant, 50 parts of ethanol solution and 20 parts of nickel for later use;

[0023] 2) Take 50 parts of ferric nitrite solution and place it in a reaction vessel, put 20 parts of nickel, 20 parts of cobalt and 20 parts of zinc into 50 parts of ferric nitrite solution, adjust the reaction temperature to be 50 degrees Celsius, and use a stirring device to stir for 1-2 hour, set the stirring frequency as one hundred and twenty revolutions per minute, and make the mixed solution 1;

[0024] 3) Add 40 parts of alumina and 10 part...

Embodiment 2

[0031] Embodiment 2: a preparation method of darunavir, comprising the following steps:

[0032] 1) Take 25 parts of cobalt, 15 parts of triethylamine, 15 parts of ferrous oxide, 15 parts of zinc oxide, 4 parts of 1.2 equivalents of hydrogen methane, 25 parts of zinc, 65 parts of ferric nitrite solution, 35 parts of metal alkali, and 45 parts of aluminum, 15 parts of silicon dioxide, 4 parts of p-acetamidobenzoyl sulfonyl chloride, 4 parts of precipitant, 65 parts of ethanol solution and 25 parts of nickel for subsequent use;

[0033] 2) Get 65 parts of ferric nitrite solution and place it in a reaction vessel, put 25 parts of nickel, 25 parts of cobalt and 25 parts of zinc into ferric nitrite solution 65, adjust the reaction temperature to be 50 degrees Celsius, and use a stirring device to stir for 1-2 hour, set the stirring frequency as one hundred and twenty revolutions per minute, and make the mixed solution 1;

[0034] 3) Add 45 parts of alumina and 15 parts of silicon ...

Embodiment 3

[0040] Embodiment three: a preparation method of darunavir, comprising the following steps:

[0041] 1) Take 30 parts of cobalt, 20 parts of triethylamine, 20 parts of ferrous oxide, 20 parts of zinc oxide, 5 parts of 1.2 equivalents of hydrogen methane, 30 parts of zinc, 80 parts of ferric nitrite solution, 40 parts of metal alkali, and 50 parts of aluminum, 20 parts of silicon dioxide, 5 parts of p-acetamidobenzoyl sulfonyl chloride, 5 parts of precipitant, 80 parts of ethanol solution and 30 parts of nickel for standby;

[0042] 2) Take 80 parts of ferric nitrite solution and place it in a reaction vessel, put 30 parts of nickel, 30 parts of cobalt and 30 parts of zinc into 80 parts of ferric nitrite solution, adjust the reaction temperature to be 50 degrees Celsius, and use a stirring device to stir for 1-2 hour, set the stirring frequency as one hundred and twenty revolutions per minute, and make the mixed solution 1;

[0043] 3) Add 50 parts of alumina and 20 parts of s...

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PUM

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Abstract

The invention relates to the technical field of medicines and discloses a method for preparing darunavir. The method comprises the following step: preparing 20-30 parts of cobalt, 10-20 parts of triethylamine, 10-20 parts of ferrous oxide, 10-20 parts of zinc oxide, 3-5 parts of 1.2 equivalent of marina hydrogen methane, 20-30 parts of zinc, 50-80 parts of a ferric nitrite solution, 30-40 parts ofa metal base, 40-50 parts of alumina, 10-20 parts of silica, 3-5 parts of p-acetamide benzoyl sulfonyl chloride, 3-5 parts of a precipitant, 50-80 parts of an ethanol solution and 20-30 parts of nickel for later use. According the method for preparing the darunavir, 20-30 parts of cobalt, 10-20 parts of triethylamine, 10-20 parts of ferrous oxide, 10-20 parts of zinc oxide, 3-5 parts of 1.2 equivalent of marina hydrogen methane, 10-20 parts of silica, 3-5 parts of p-acetamide benzoyl sulfonyl chloride, 3-5 parts of the precipitant, 50-80 parts of the ethanol solution and 20-30 parts of nickelare adopted for later use, the reaction materials used in the method are low in price and low in reaction environment requirement, correspondingly, the preparation cost of the darunavir is greatly reduced, patients can afford the darunavir, and the darunavir can truly benefit the patients.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical production, in particular to a preparation method of darunavir. Background technique [0002] Darunavir is a non-peptide HIV protease inhibitor, which works by blocking the formation of new, mature virion particles released from the surface of infected host cells and inhibiting viral protease. When this product is used for a long time Usually, it can reduce the HIV virus carrier in the blood, increase the count of CD4 cells, reduce the chance of AIDS infection, improve the quality of life, and prolong life. adults. [0003] The preparation route of darunavir has been disclosed for a long time, but in the disclosed route method, the preparation efficiency of darunavir is low, the preparation cost is high, and the requirements for the preparation environment are also high, resulting in the price of darunavir finally prepared High, patients cannot afford such a high price, and the promotion ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/04
CPCC07D493/04
Inventor 徐军蒋信义张敏华周宇
Owner ABA CHEM CORP
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