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Synthetic method of drug lamotrigine for curing bipolar disorder and epilepsy

A technology of bipolar affective disorder and lamotrigine, which is applied in the direction of organic chemistry, can solve the problems of complex production process, unsuitable for large-scale production, harsh reaction conditions, etc., and achieve high raw material utilization rate, high social and economic benefits , the effect of fewer reaction steps

Inactive Publication Date: 2012-11-07
SANJIN GROUP HUNAN SANJIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The existing lamotrigine preparation method is lengthy and the yield is low. The preparation process needs to use a large amount of toxic substances, and the reaction conditions are harsh. At the same time, a large amount of toxic substances will be produced, which will not only pollute the environment, but also cause harm to the human body, such as : the ZL201010516051.1 that has been published in the patent literature, the preparation method, the reaction process reaches several steps, will use toxic and harmful substances such as oleum, 2,3-dichlorobenzoyl cyanide, low yield, large production The process is complicated; as the preparation method described in ZL200780030010.8, the preparation process needs to be completed under acidic and alkaline conditions, and microwave heating is used in the reaction process, which is not suitable for large-scale production

Method used

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  • Synthetic method of drug lamotrigine for curing bipolar disorder and epilepsy
  • Synthetic method of drug lamotrigine for curing bipolar disorder and epilepsy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: First put 2-cyano-(2,3-dichlorophenyl)-2-guanidine iminoacetonitrile and n-propanol into the reaction tank at a ratio of 1:5, heat up and stir, and the reaction temperature reaches 65 0 C. After all the reactants are dissolved, time the reaction for 5 hours. After the reaction is completed, the solution is cooled to 5 0 8 hours of crystallization at C, filtered to obtain the crude product of lamotrigine, about 40% of moisture; then the crude product of lamotrigine was dropped into the refining tank, added 10 times the amount of n-propanol of the crude product of lamotrigine, stirred and heated up to 65 0 Above C, the crude product of lamotrigine is completely dissolved, and the temperature is lowered to 50 0 After C, add gac, add-on is 5% of lamotrigine crude product weight, stirring and reflux decolorization 30 minutes, filter while hot then, when filtrate is cooled to normal temperature, in 5 0 Crystallize at C for 10 hours; finally filter to obtain the w...

Embodiment 2

[0020] Example 2: Put 2-cyano-(2,3-dichlorophenyl)-2-guaniminoacetonitrile and n-propanol into the reaction tank at a ratio of 1:20, heat up and stir, and the reaction temperature reaches 60 0 C, reflux timing reaction for 8 hours, the reaction is completed, filtered while hot, and the filtrate is cooled to 10 0 C crystallized for 2 hours, filtered to obtain the wet crude product of lamotrigine, with a moisture content of about 40%; put the wet crude product of lamotrigine into the refining tank, add 5 times the amount of n-propanol solution of the crude wet product, and stir to heat up to 70 0 C reflux to dissolve all the crude product of lamotrigine and cool to 50 0 C, adding activated carbon, the addition is 10% of the crude product weight of lamotrigine, stirred and refluxed for decolorization for 0.5 hour, filtered while hot, and the filtrate was cooled at 10 0 C for 0.5 hours of crystallization, and finally filtered to obtain the wet product of lamotrigine, which was dr...

Embodiment 3

[0021] Example 3: First put 2-cyano-(2,3-dichlorophenyl)-2-guanidine iminoacetonitrile and n-propanol into the reaction tank at a ratio of 1:10, heat up and stir, and the reaction temperature reaches 90 0 C. After all the reactants are dissolved, time the reaction for 0.5 hours. After the reaction is completed, the solution is cooled to 20 0 0.5 hours of crystallization at C, filtered to obtain the crude product of lamotrigine, about 40% of moisture; then the crude product of lamotrigine was dropped into the refining tank, added 20 times the amount of n-propanol of the crude product of lamotrigine, stirred and heated up to 60 0 C, the crude product of lamotrigine is completely dissolved, and the temperature is lowered to 40 0 After C, add gac, add-on is 8% of lamotrigine crude product weight, stirring and reflux decolouring 30 minutes, filter while hot then, when filtrate is cooled to normal temperature, at 8 0 Crystallize at C for 3 hours; finally filter to obtain the wet r...

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Abstract

The invention provides a synthetic method of drug lamotrigine for curing bipolar disorder and epilepsy. 2-cyano-(2, 3-dichlorophenyl)-2-guanidine amino acetonitrile and n-propyl alcohol (CH3CH2CH2OH) solvent are used as a raw material, and the lamotrigine is generated through one-step cyclization reaction in a reaction tank. The synthetic method of the drug lamotrigine includes material preparation, crude product manufacturing, purification, filtration and drying. The raw material of the synthetic method comprises only the 2-cyano-(2, 3-dichlorophenyl)-2-guanidine amino acetonitrile as a starting material and the n-propyl alcohol (CH3CH2CH2OH) solvent and has no strong acid, strong base and other toxic substances, the lamotrigine is manufactured through the one-step cyclization reaction, and therefore the synthetic method is small in reaction steps, high in yield, simple and convenient to operate and high in raw material utilization rate, avoids using toxic and harmful substances in abundance, reduces production cost remarkably, and has high social benefits and social benefits.

Description

technical field [0001] The invention relates to a preparation method of western medicine, in particular to a synthesis method of lamotrigine, a drug for treating bipolar affective disorder and epilepsy. Background technique [0002] The medical community believes that epilepsy is a central nervous system disease that is difficult to cure and requires life-long medication. The incidence rate of epilepsy in my country is 0.5%-0.8%, and there are about 10 million active epilepsy patients in the country; with the competition of people in the society Increasingly intense, increased work or ideological pressure, or personal emotional disorders have increased the number of people suffering from depression. According to a survey by the Psychiatric Branch of the Chinese Medical Association, there are more than 20 million depressed patients in my country, and the U.S. FDA In 2003, the indication of lamotrigine for the treatment of bipolar disorder was approved, so the technical developm...

Claims

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Application Information

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IPC IPC(8): C07D253/075
Inventor 杨银芝陈林张宇
Owner SANJIN GROUP HUNAN SANJIN PHARMA
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