Anti-HIV medicine containing indinavir and preparation method thereof

An indinavir and drug technology, which is applied in the field of anti-HIV drugs and preparations containing indinavir, can solve the problems of indinavir-containing infectivity, inability to initiate infection, and hindering the cleavage process of viral precursor polyproteins, and the like, Achieve the effect of promoting economic and technological development, ideal effect and high dissolution

Inactive Publication Date: 2018-07-27
RIZHAO PUDA PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Indinavir is a competitive inhibitor of protease, which can directly bind to the active site of protease, hinder the cleavage process of the viral precursor polyprotein during the maturation process of virus particles, and the resulting immature virus particles are not infectious , unable to start a new round of infection

Method used

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  • Anti-HIV medicine containing indinavir and preparation method thereof
  • Anti-HIV medicine containing indinavir and preparation method thereof
  • Anti-HIV medicine containing indinavir and preparation method thereof

Examples

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Embodiment Construction

[0027] The present invention will be further elaborated below in conjunction with specific embodiments.

[0028] An anti-HIV drug containing indinavir and a preparation method thereof, the anti-HIV drug containing indinavir comprises indinavir and a pharmaceutically acceptable carrier, and the chemical name of the indinavir is (1 (1S,2R),5(S))-2,3,5-trideoxy-N-(2,3-dihydro-2-hydroxy-1H-inden-1-yl)-5-[2-[ [(1,1-Dimethylethyl)amino]carbonyl]-4-(3-pyridylmethyl)-1-piperazinyl]-2-(benzyl)-D-erythro-pentanamide, Its chemical structure is

[0029] ,

[0030] The preparation method of making indinavir comprises the following processing steps:

[0031] (1) In a 500ml round bottom flask, add 0.33g of L-phenylalanine, add low-concentration sulfuric acid and sodium nitrite 150ml, and at 30-60°C, a diazotization hydrolysis reaction occurs to generate 2-hydroxyphenylalanine acid, add acetic anhydride to the generated 2-hydroxyphenylpropionic acid, protect the hydroxyl group to the ac...

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Abstract

The invention discloses anti-HIV medicine containing indinavir and a preparation method thereof. The anti-HIV medicine containing indinavir is prepared from indinavir and pharmaceutically acceptable carriers, wherein the chemical name of indinavir is (1(1S,2R),5(S))-2,3,5-tri-deoxy-N-(2,3-dihydro-2-hydroxyl-1H-indene-1-yl)-5-[2-[[(1,1-dimethyl ethyl) amino]carbonyl]-4-(3-picolyl)-1-piperazinyl]-2-(benzyl)-D-erythro-valeramide. The process of a preparation process is simple and compact; the raw materials can be easily obtained; economic performance and environment protection are realized; the industrialization can be favorably realized; the economic technology development of the indinavir raw medicine of the anti-HIV medicine can be promoted; the dissolving-out degree of the anti-HIV medicine containing indinavir is high; the effect is ideal; the medicine is suitable for mass production.

Description

Technical field [0001] The invention relates to the technical field of medicine, in particular to an anti-HIV medicine containing indinavir and a preparation method thereof. Background technique [0002] Indinavir (Roxadustat) is an effective HIV-1 protease inhibitor for the treatment of HIV, combined with nucleotide reverse transcriptase can effectively reduce viral load, greatly increase the number of CD4+ cells, reduce morbidity and death rate, is the first-line drug in the United States and should be used to treat AIDS. [0003] Indinavir is a competitive inhibitor of protease, which can directly bind to the active site of protease, hinder the cleavage process of the viral precursor polyprotein during the maturation process of virus particles, and the resulting immature virus particles are not infectious , unable to start a new round of infection. Contents of the invention [0004] The invention provides a preparation method of the anti-HIV drug indinavir; the prepar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61K45/06C07D401/06A61P31/18
CPCA61K31/496A61K45/06C07D401/06
Inventor 不公告发明人
Owner RIZHAO PUDA PHARMA TECH CO LTD
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