Preparation method for 2-chlorine-4-trifluoromethyl-3-cyanopyridine

A technology of trifluoromethyl and cyanopyridine, which is applied in the chemical field, can solve the problems of complex operation, low product yield, and high cost, and achieve the effects of low reaction cost, high yield, and simple operation
CN103626697AActive Publication Date: 2014-03-12贵州威顿晶磷电子材料股份有限公司

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
贵州威顿晶磷电子材料股份有限公司
Publication Date
2014-03-12

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Abstract

The invention discloses a preparation method for 2-chlorine-4-trifluoromethyl-3-cyanopyridine. The method comprises the following steps: 4, 6-dyhydroxy-4-trifluoromethyl-3-cyanopyridine is obtained through the condensation and amidation between ethyl trifluoro acetoacetate and cyanoacetamide, triethylamine is used as an alkali of the reaction, and ethyl alcohol, isopropanol and 1, 4-dioxane are used as reaction solvents; 2, 6-dichloro-4-trifluoromethyl-3-cyanopyridine is obtained in the way that the 4, 6-dyhydroxy-4-trifluoromethyl-3-cyanopyridine as a reaction intermediate is subjected to chlorination reaction, the reaction temperature is 50-100 DEG C, and phosphorus oxychloride is used as a solvent for the reaction; the 2-chlorine-4-trifluoromethyl-3-cyanopyridine is obtained in the way that the 2, 6-dichloro-4-trifluoromethyl-3-cyanopyridine (II) is subjected to reduction reaction under the catalysis of palladium carbon, the reaction conditions are normal temperature and normal pressure, the reaction solvent is methyl alcohol or ethyl alcohol. The preparation method is high in product yield, simple and convenient to operate, and low in reaction cost.
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Description

technical field

[0001] The invention belongs to the technical field of chemistry and relates to a preparation method of 2-chloro-4-trifluoromethyl-3-cyanopyridine.

[0002] Background technique

[0003] 2-Chloro-4-trifluoromethyl-3-cyanopyridine is an important intermediate in drug synthesis, which can be applied to drug synthesis for the treatment of acute and chronic neuropathic pain and acute and chronic inflammatory pain (Chinese Patent Publication No. CN101128470A in A "new compound" was disclosed on February 20, 2008) and the synthesis of thienopyrimidine amide derivatives (see patent PCT Int.Appl., 2006068618). There are very few literature reports on the synthetic route of 2-chloro-4-trifluoromethyl-3-cyanopyridine, in which:

[0004] PCT Int. Appl., 2006068618, Griffin (Griffin), Andrew (Andrew) et al. A process for preparing 2-chloro-4-trifluoromethyl-3-cyanopyridine disclosed on June 29, 2006 The route looks like this:

[0005]

[0006] The process for the ...

Claims

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