Preparing method for tiagabine hydrochloride

A technology of tiagabine hydrochloride and tiagabine ethyl ester, which is applied in the field of preparation of tiagabine hydrochloride, can solve the problems of waste of materials, increase of production cost, low yield, etc., and achieve the effect of simple operation and increased yield
CN103351384AActive Publication Date: 2013-10-16凯默斯医药科技上海有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
凯默斯医药科技上海有限公司
Publication Date
2013-10-16

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Abstract

The invention provides a preparing method for tiagabine hydrochloride, which includes the following operating steps: firstly, taking tiagabine ethyl ester to be dissolved in solvent, adding L-configuration organic acid, performing heating reflux until the tiagabine ethyl ester is completely dissolved, then performing reflux for 30-60 min, cooling to the room temperature, cooling and crystallizing at the temperature of minus 30 -minus 20 DEG C, and collecting a solid matter A; secondly, adding solvent in the solid matter A, performing heating reflux until the tiagabine ethyl ester is completely dissolved, then performing reflux for 30-60 min, cooling to the room temperature, cooling and crystallizing at the temperature of minus 10-0 DEG C, and collecting a solid matter B; thirdly, dissolving the solid matter B, sequentially adding sodium hydroxide and hydrochloric acid to react, extracting and recrystallizing, so as to obtain the tiagabine hydrochloride. The preparing method provided by the invention not only remarkably improves the productivity by 90% above, but also guarantees the 99.9% of chemical and optical purity, is simple and convenient to operate, has no special requirement for equipment, and is more suitable for large-scale industrial production.
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Description

technical field

[0001] The present invention relates to a preparation method of tiagabine hydrochloride. Background technique

[0002] Tiagabine (Formula 1) is a GABA reuptake inhibitor developed by Novo Nordisk in Denmark in 1997 and marketed in the United States and the United Kingdom in 1998. It can be used to treat partial seizures and grand mal seizures of epilepsy. As well as seizures that cannot be controlled by other antiepileptic drugs, it has the characteristics of good tolerance, small side effects and suitable for long-term use. In terms of mechanism of action, as a selective and reversible inhibitor of GABA reuptake in neurons and glial cells, tiagabine mainly inhibits mediator transmission in the central nervous system, increases the concentration of GABA in synapses, and reduces the sensitivity of neural excitation. , improve clinical. As a single optical isomer, the pharmacological activity of tiagabine in the R-configuration is much greater than that in th...

Claims

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