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Method for preparing nevirapine

A technology of nevirapine and its compound, which is applied in the new field of preparation of nevirapine (Nevirapine), can solve problems such as environmental pollution, and achieve the effects of reducing safety hazards, low toxicity, and low price

Inactive Publication Date: 2011-08-31
HUNAN BOAODE BIOPHARML TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The advantage of this method is that it avoids the high-pressure reaction, but on the one hand, it uses phosphorus oxychloride or thionyl chloride, which is highly irritating and volatile, as the acid chloride reagent, and on the other hand, it uses sodium hydride or expensive hexamethyl Disilicon amide sodium as a strong base is likely to cause environmental pollution

Method used

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  • Method for preparing nevirapine
  • Method for preparing nevirapine
  • Method for preparing nevirapine

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Experimental program
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Embodiment Construction

[0037]

[0038] Synthesis of Compound IV:

[0039] In the reaction flask, add 157.5 g (1.00 mol) of 2-chloronicotinic acid (compound II), 1000 ml of ethanol, 92.4 g (1.10 mol) of sodium bicarbonate and 500 ml of water, stir at room temperature for 30 minutes, and add 114 g of cyclopropylamine ( 2.0mol), heat up to 50°C and react for 24 hours. After the reaction, concentrate under reduced pressure to remove unreacted cyclopropylamine, ethanol and water to a volume of about 400ml, add 200ml of ethyl acetate for extraction, separate layers, and cool down the water layer To 0-5°C, add 4N hydrochloric acid dropwise to adjust PH=4-5, solid precipitates, stand for 2 hours, filter, filter cake is washed with ice water, and dried to obtain 152.8 g of yellow solid, yield 85.82% (based on compound II calculation).

[0040] 1HNMR (300MHz, CDCl3): δ (ppm) 0.35-0.52 (m, 4H), 1.32-1.36 (m, 1H),

[0041] 6.70-6.73 (m, 1H), 7.82-7.86 (m, 1H), 8.30-8.33 (m, 1H).

[0042] Synthesis of co...

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Abstract

The invention discloses a method for preparing nevirapine, in particular a new method for preparing a non-nucleoside reverse transcriptase inhibitor of Nevirapine for treating human immunodeficiency virus (HIV). The method comprises the following steps of: reacting 2-chloronicotinic acid serving as an initial material with cyclopropanamine; performing amidation reaction with 2-chloro-3-amino-4-methyl pyridine in the presence of N-hydroxysuccinimide, dicyclohexylcarbodiimide and triethylamine; and closing a ring under the action of potassium tert-butoxide to obtain the Nevirapine. The method has the advantages of cheap and readily available raw materials, simple operation, light pollution and suitability for industrial production.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a new preparation method of Nevirapine. Background technique [0002] Nevirapine, the chemical name is 11-cyclopropyl-5,11-dihydro-4-methyl-6H-dipyrido[3,2-b:2',3'-e]diazepine -6-ketone is the first non-nucleoside reverse transcriptase inhibitor for the treatment of HIV, developed by Boehringer Ingelheim in Germany and first listed in the United States in 1996. [0003] Nevirapine prevents the replication of HIV by directly linking with HIV reverse transcriptase, thereby reducing the amount of virus in the body. For pregnant women who have not used antiretroviral therapy during delivery, the application of nevirapine can prevent mother-to-child transmission of HIV-1. [0004] At present, there are mainly three types of methods for the preparation of nevirapine: [0005] First class method: [0006] [0007] These methods all adopt 2-chloro-3-amino-4-picoline and 2-chloronicotinyl ch...

Claims

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Application Information

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IPC IPC(8): C07D471/14
Inventor 林开朝李兴民陶友妮
Owner HUNAN BOAODE BIOPHARML TECH DEV
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