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A process of synthesizing praziquantel

A process method and a technology for praziquantel, applied in the field of synthesizing praziquantel, can solve the problems of high production cost, high price, complicated process and the like in the process of synthesizing praziquantel, and achieve a simple and controllable operation method, high economic value, and environmental protection. good safety effect

Inactive Publication Date: 2017-06-20
JIANGSU CHENGXIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The existing synthetic praziquantel process has high production cost, complex process, low yield, heavy pollution, relatively dangerous operation, serious discharge of three wastes and other factors, and the price is relatively expensive

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] 1.1 Put 12.g (0.1mol) of β-phenylethylamine and 120g of dichloromethane into the reaction kettle, stir and cool to below 0-5°C. 11.3g (0.1mol) of chloroacetyl chloride and 13.3g (0.1mol) of liquid caustic soda were added dropwise to the reaction liquid under temperature control, and the pH value was controlled to be 6 during the dropwise addition. Intermediate 1.

[0026] 1.2 Add 10.5g (0.1mol) of amino substances to the BK-1 dichloromethane solution. Insulate the reaction for 2.0 hours, control the internal temperature not to exceed 60°C and recover the amino compound by distillation under reduced pressure until no fraction is distilled to obtain the praziquantel intermediate 2.

[0027] 1.3 Put praziquantel intermediate 2 and 120 g of dichloromethane into the reaction kettle, keep the temperature in the reaction bottle below 10-15°C and add 10.0 g (0.1 mol) of concentrated sulfuric acid dropwise to carry out the ring closure reaction. The praziquantel intermediate 3...

Embodiment 2

[0030] 1.1 Put 12.g (0.1mol) of β-phenylethylamine and 120g of dichloromethane into the reaction kettle, stir and cool to below 0-10°C. Add 17.0 g (0.15 mol) of chloroacetyl chloride and 14.6 g (0.11 mol) of liquid caustic soda dropwise to the reaction liquid under temperature control, control the pH value to 7 during the dropping process, keep stirring after the dropping, and separate layers to obtain praziquantel Intermediate 1.

[0031] 1.2 Add 21.0 g (0.2 mol) of amino substances to the BK-1 dichloromethane solution. Insulate the reaction for 2.0 hours, control the internal temperature not to exceed 60°C and recover the amino compound by distillation under reduced pressure until no fraction is distilled to obtain the praziquantel intermediate 2.

[0032] 1.3 Put the praziquantel intermediate 2 and 120g of dichloromethane into the reaction kettle, keep the temperature in the reaction bottle below 10-20℃, add 10.0g (0.1mol) of concentrated sulfuric acid dropwise to carry ou...

Embodiment 3

[0035] 1.1 Put 12.g (0.1mol) of β-phenylethylamine and 120g of dichloromethane into the reaction kettle, stir and cool to below 10-20°C. Add 17.0 g (0.15 mol) of chloroacetyl chloride and 14.6 g (0.11 mol) of liquid caustic soda dropwise to the reaction liquid under temperature control, control the pH value to 7 during the dropping process, keep stirring after the dropping, and separate layers to obtain praziquantel Intermediate 1.

[0036] 1.2 Add 10.5g (0.1mol) of amino substances to the BK-1 dichloromethane solution. Insulate the reaction for 2.0 hours, control the internal temperature not to exceed 100°C and recover the amino compound by distillation under reduced pressure until no fraction is distilled to obtain the praziquantel intermediate 2.

[0037] 1.3 Put the praziquantel intermediate 2 and 120g of dichloromethane into the reaction kettle, keep the temperature in the reaction bottle below 10-20℃, add 10.0g (0.1mol) of concentrated sulfuric acid dropwise to carry ou...

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PUM

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Abstract

A process of synthesizing praziquantel is provided. According to the process, beta-phenylethylamine and dichloromethane are added into a reactor and subjected to an acylation reaction; the mixture is stirred and cooled and the acylation reaction temperature is lowered to 0-35 DEG C or below; chloroacetyl chloride and liquid caustic soda are added dropwise under temperature control of the reaction solution; the pH value of the acylation reaction solution is controlled to be 6-12 during a dropwise adding procedure; and after the dropwise adding procedure is finished, the temperature is maintained, and the mixture is stirred and layered. A one-pot method is adopted by the process, the cost of the process is low, operation methods are simple and controllable, environment protection safety is good and product quality is stable.

Description

technical field [0001] The invention relates to a process for synthesizing praziquantel, which belongs to the technical field of medicine and its intermediates. Background technique [0002] Praziquantel is a broad-spectrum anti-parasitic drug, which is very effective against major human schistosomiasis. Since it was first launched in Germany in 1980, it has quickly become the first choice drug for the treatment of schistosomiasis and various parasitic diseases in the world. The advent of praziquantel is a major breakthrough in the treatment of parasitic diseases. At present, it has become the most widely used anti-parasitic drug in the world. [0003] The existing process for synthesizing praziquantel has high production cost, complex process, low yield, heavy pollution, relatively dangerous operation, serious discharge of three wastes and other factors, and the price is relatively expensive. Contents of the invention [0004] Purpose of the invention: In order to overco...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04
CPCC07D471/04
Inventor 吴锋祝俊刘家生华俊国刘双喜王子坤邢小飞潘红强
Owner JIANGSU CHENGXIN PHARMA
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