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Method for preparing nevirapine

A nevirapine and reaction technology, applied in the field of biopharmaceuticals, can solve the problems of unsuitability for industrialized production, high production cost, harsh process conditions, etc., and achieve the effects of low cost, good quality and good production prospects

Inactive Publication Date: 2013-03-06
KAMP PHARMA
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  • Summary
  • Abstract
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AI Technical Summary

Problems solved by technology

[0009] This synthesis method needs low temperature reaction, the process conditions are harsh, and the actual production cost is high. It is not suitable for industrial production and is only suitable for laboratory preparation.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0030] (1) Preparation of 2,6-dihydroxy-3-cyano-4-methylpyridine:

[0031] Add cyanoacetamide (84g, 1mol), ethyl acetoacetate (130g, 1mol) and methanol (200ml) in 1L three-necked flask, add potassium hydroxide (68.4g, 1.2mol) methanol (200ml) dropwise at 68°C The solution was dropped within 2 hours, and refluxed at the same temperature for 8 hours. Cool to room temperature, filter, transfer the filtrate to a 3L flask, add water (1.2L) at 70°C, acidify with concentrated hydrochloric acid (80ml) after complete dissolution, and a large amount of white solid precipitates out. Filter and dry the filter cake to obtain white powder 2,6-dihydroxy-3-cyano-4-methylpyridine (144.5 g, 96.3%).

[0032] (2) Preparation of 2,6-dichloro-3-cyano-4-methylpyridine:

[0033] Add 2,6-dihydroxy-3-cyano-4-methylpyridine (150g, 1mol) and phosphorus oxychloride (485ml, 5.3mol) into a 2L autoclave, heat to 130°C and stir for 8h after decompression . After the reaction, the material was poured into ...

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PUM

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Abstract

The invention relates to a method for preparing nevirapine. With the method disclosed by the invention, the nevirapine is obtained in four steps of Knoevenagel reaction, amination, copper salt catalytic reaction and cyclizing. The method has the advantages of simple technology and convenience in operation and is suitable for the large scale production of the modern enterprise, and the obtained nevirapine has an important influence on the development of the medicine field, and has a huge economic value and social value.

Description

technical field [0001] The invention relates to the field of biopharmaceuticals, in particular to a preparation method of nevirapine. Background technique [0002] Nevirapine, NVP for short, chemical name is 11-cyclopropyl-4-methyl-5,11-dihydro-4-methyl-6H-dihydropyrido[3,2-b:2′, 3′-e][1,4]diazepine-6-one, molecular formula is C 15 h 14 N 4 O, with a relative molecular weight of 266.30, is a non-nucleoside HIV reverse transcriptase inhibitor developed by Boehringer Ingelheim, Germany. Its mechanism of action is to directly connect with HIV reverse transcriptase and break the catalytic end of the enzyme to block the activity of RNA-dependent and DNA-dependent DNA polymerase, thereby effectively reducing the number of viruses in the body and restoring human immune function. In September 1996, nevirapine was approved for marketing by the US FDA, and in 1998 the US FDA approved the expansion of indications. Nevirapine is one of the widely used drugs for the treatment and pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/14
Inventor 杨述朱敏吴健民
Owner KAMP PHARMA
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