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Preparation method of darunavir

A darunavir, equivalent technology, applied in the field of preparation of darunavir, can solve the problems of complex preparation methods, loss of consumables, and high requirements for the preparation environment of darunavir, so as to achieve low requirements for the preparation environment and not easy to waste consumables , Ease of use

Inactive Publication Date: 2018-11-16
ABA CHEM NANTONG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Aiming at the deficiencies in the prior art, the present invention provides a preparation method of darunavir, which has the advantages of simple preparation method, etc., and solves the problem that the traditional preparation method of darunavir is relatively complicated, and the preparation environment of darunavir The requirements are relatively high. Users need to use complicated preparation equipment and a variety of fine materials when preparing darunavir. Users often need to concentrate and be careful when preparing darunavir. A momentary mistake will lead to Failure to take it, all previous efforts were wasted, and a large amount of consumables were lost. Users are very troubled by this problem.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Embodiment one: a kind of preparation method of darunavir comprises the following steps:

[0019] 1) Now take 20 mg of N-dibenzyl-L-phenylalanine methyl ester, 40 mg of N-hydroxyl compound, 20 mg of 1 equivalent of cyanohydromethane, 100 mg of butyllithium, 50 mg of tetrahydrofuran solvent, amines 70 mg, (2S,3R)-2-amino-4-fluoro-1-phenylbutan-3-ol 60 mg, halogenated aromatic ring 40 mg, triethylamine and difluoromethane 10 mg, 1.3 equivalents of di 5 mg of di-tert-butyl carbonate and 20 mg of metal base are prepared, 20 mg of N-dibenzyl-L-phenylalanine methyl ester, 40 mg of N-hydroxyl compound, 20 mg of 1 equivalent of cyanohydromethane, butyl Lithium base 100 mg, tetrahydrofuran solvent 50 mg and amines 70 mg were placed in an environment of minus 20 degrees Celsius for use, (2S, 3R)-2-amino-4-fluoro-1-phenylbutan-3-ol 60 mg, halogen 40 mg of substituting aromatic ring, 10 mg of triethylamine and difluoromethane, 5 mg of 1.3 equivalents of di-tert-butyl dicarbonate a...

Embodiment 2

[0025] Embodiment 2: a preparation method of darunavir, comprising the following steps:

[0026] 1) Now take 25 mg of N-dibenzyl-L-phenylalanine methyl ester, 65 mg of N-hydroxyl compound, 30 mg of 1 equivalent of cyanohydromethane, 125 mg of butyllithium, 65 mg of tetrahydrofuran solvent, amines 90 mg, (2S,3R)-2-amino-4-fluoro-1-phenylbutan-3-ol 80 mg, halogenated aromatic ring 50 mg, triethylamine and difluoromethane 15 mg, 1.3 equivalents of di 12.5 mg of di-tert-butyl carbonate and 30 mg of metal base are prepared, 25 mg of N-dibenzyl-L-phenylalanine methyl ester, 65 mg of N-hydroxy compound, 30 mg of 1 equivalent of cyanohydromethane, butyl Lithium base 125 mg, tetrahydrofuran solvent 65 mg and amines 90 mg are placed in the environment of minus 20 degrees Celsius for standby, (2S, 3R)-2-amino-4-fluoro-1-phenylbutan-3-ol 80 mg, halogen 50 mg of substituting aromatic ring, 15 mg of triethylamine and difluoromethane, 12.5 mg of 1.3 equivalents of di-tert-butyl dicarbonate ...

Embodiment 3

[0032] Embodiment three: a preparation method of darunavir, comprising the following steps:

[0033] 1) Now take 30 mg of N-dibenzyl-L-phenylalanine methyl ester, 90 mg of N-hydroxyl compound, 40 mg of 1 equivalent of cyanohydromethane, 150 mg of butyllithium, 80 mg of tetrahydrofuran solvent, amines 110 mg, (2S, 3R)-2-amino-4-fluoro-1-phenylbutan-3-ol 100 mg, halogenated aromatic ring 60 mg, triethylamine and difluoromethane 20 mg, 1.3 equivalents of di 20 mg of di-tert-butyl carbonate and 40 mg of metal base are prepared, 30 mg of N-dibenzyl-L-phenylalanine methyl ester, 90 mg of N-hydroxyl compound, 40 mg of 1 equivalent of cyanohydromethane, butyl Lithium base 150 mg, tetrahydrofuran solvent 80 mg and amines 110 mg were placed in the environment of minus 20 degrees Celsius for standby, (2S, 3R)-2-amino-4-fluoro-1-phenylbutan-3-ol 100 mg, halogen 60 mg of substituting aromatic ring, 20 mg of triethylamine and difluoromethane, 20 mg of 1.3 equivalents of di-tert-butyl dicar...

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PUM

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Abstract

The invention relates to the technical field of chemical engineering and discloses a preparation method of darunavir, which includes a step of preparing raw materials comprising: 20-30 mg of N-dibenzyl-L-methyl phenylalanine ester, 40-90 mg of a N-hydroxyl compound, 20-40 mg of Binqing methane in 1 equivalent, 100-150 mg of butyl lithium, 50-80 mg of a tetrahydrofuran solvent, 70-110 mg of amines,60-100 mg of (2S,3R)-2-amino-4-chloro-phenylbutane-3-ol, 40-60 mg of a halogenated aromatic ring compound, 10-20 mg of triethylamine and dichloromethane, 5-20 mg of di-tert butyl dicarbonate in 1.3 equivalents, and 20-40 mg of metal alkali; and preserving 20-30 mg of the N-dibenzyl-L-methyl phenylalanine ester, 20-40 mg of the Binqing methane in 1 equivalent, 100-150 mg of the butyl lithium and 70-110 mg of the amines at -20 DEG C for later use. The preparation method is low in demand on environment, avoids complex operations in conventional preparation methods, is easier to prepare the darunavir and is not liable to cause waste on consumables, so that the method is convenient to carry out.

Description

technical field [0001] The invention relates to the technical field of chemical engineering, in particular to a preparation method of darunavir. Background technique [0002] Darunavir, a new non-peptide antiretroviral protease inhibitor for HIV treatment, inhibits viral proteases by blocking the formation of new, mature virions released from the surface of infected host cells And it works. When this product is used for a long time, it can usually 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. It is suitable for people infected with HIV but taking existing medicines. Adults who have not responded to antiretroviral drugs. [0003] The traditional preparation method of darunavir is relatively complicated, and the requirements for the preparation environment of darunavir are relatively high. When preparing darunavir, users need to use complicated preparation equipme...

Claims

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Application Information

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IPC IPC(8): C07D493/04
CPCC07D493/04
Inventor 蒋信义徐军刘汝章
Owner ABA CHEM NANTONG
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