Synthesis method for Nevirapine intermediates

A synthetic method and intermediate technology, applied in the field of intermediate synthesis, can solve the problems of complex reaction processing, environmental damage, etc., and achieve the effects of high yield, reduced pollution, and low cost
CN102952068AInactive Publication Date: 2013-03-06上海思协化工科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
上海思协化工科技有限公司
Publication Date
2013-03-06
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a synthesis method of a nevirapine intermediate 2-amino-3-nitro-4-methylpyridine shown as the chemical formula I. The synthesis method includes steps: under catalysis of inorganic base or organic base and actions of concentrated sulphuric acid and dilute nitric acid, subjecting the 2-amino-3-nitro-4-methylpyridine shown as the chemical formula I to nitration reaction in organic solvent. The inorganic base can be calcium hydroxide, barium hydroxide, sodium hydroxide or zinc hydroxide; and the organic base can be sodium methoxide, potassium methoxide, sodium ethoxide, potassium ethoxide, sodium tert-butoxide or potassium tert-butylate. The invention further discloses a synthesis method of a nevirapine intermediate 2-chloro-N-(2-chloro-4-methylpyridin-3-yl)nicotinamide. The synthesis method is easy and safe in operation, high in yield, low-cost, low in pollution to environments and suitable for industrial production in scale.
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Description

technical field

[0001] The present invention specifically relates to a synthetic method of an intermediate of nevirapine. Background technique

[0002] 2-Chloro-N-(2-chloro-4-methylpyridin-3-yl)nicotinamide is an important intermediate for the synthesis of nevirapine. Nevirapine is an anti-AIDS drug developed by Boehringer Ingelheim in Germany to prevent mother-to-child transmission of HIV. Nevirapine is a non-nucleoside reverse transcriptase inhibitor (Non-Nucleoside Reverse Transcriptase Inhibitor, NNRTI) of HIV-1. Nevirapine is directly linked to the reverse transcriptase of HIV-1 and blocks RNA-dependent and DNA-dependent DNA polymerase activity by breaking the catalytic end of the enzyme, thereby effectively reducing the number of viruses in the body and restoring human immune function. Nevirapine is currently one of the most widely used anti-AIDS drugs, mainly for the prevention and treatment of mother-to-child virus transmission. Therefore, it is of great significa...

Claims

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