Synthesis method of 2-fluoro-4-nitrobenzonitrile

A technology of nitrobenzonitrile and synthetic method, which is applied in the field of synthesis of 2-fluoro-4-nitrobenzonitrile, and can solve the problem of lack of 2-fluoro-4-nitrobenzonitrile reaction conditions and yield, etc. problems, to achieve the effect of reducing production costs
CN101648890BActive Publication Date: 2012-07-25CHANGZHOU XIAOGUO INFORMATION SERVICES
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
CHANGZHOU XIAOGUO INFORMATION SERVICES
Publication Date
2012-07-25

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Abstract

The invention relates to a synthesis method of 2-fluoro-4-nitrobenzonitrile and the method comprises the following steps: adopting 2-fluoro-4-nitrophenylamine as raw material, using diazotization bromination to convert -NH2 in 2-fluoro-4-nitrophenylamine to -Br and then using NMP as solvent to perform cyaniding and obtain 2-fluoro-4-nitrobenzonitrile. The invention has the advantage of cheap and accessible raw material, lower toxicity of raw material and capability of industrialized production.
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Description

1. Technical field

[0001] The invention relates to a synthesis method of 2-fluoro-4-nitrobenzonitrile, in particular to a drug intermediate which can be used as an irreversible inhibitor of tyrosine kinase. 2. Background technology

[0002] The English name of 2-fluoro-4-nitrobenzonitrile is 2-Fluoro-4-nitrobenzonitrile, and the molecular formula is C 7 h 3 FN 2 o 2 , is a pharmaceutical intermediate, a pharmaceutical intermediate that can be used as an irreversible inhibitor of tyrosine kinase, which can be used to treat diseases such as cancer, atherosclerosis, restenosis, endometriosis or psoriasis .

[0003] At present, there are four main methods for synthesizing 2-fluoro-4-nitrobenzonitrile:

[0004] 1. First oxidize 2-fluoro-4-nitrotoluene to 2-fluoro-4-nitrobenzoic acid, then to 2-fluoro-4-nitrobenzamide, and finally to 2-fluoro-4-nitrotoluene benzonitrile;

[0005]

[0006] Among them, the paper "Exploiting Subsite S1 of Trypsin-Like Serine Proteases for S...

Claims

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