Method for preparing nevirapine

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...

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