Synthesis method of Gabitril and its racemate and S-configuration

A synthesis method and racemate technology, which are applied in the preparation of ethyl β-piperidinecarboxylate, tiagabine and S-configuration tiagabine, can solve the problems of unsuitability for industrial production and high price, and achieve The effect of convenient operation and mild reaction conditions
CN1288145CInactive Publication Date: 2006-12-06SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
Publication Date
2006-12-06
Estimated Expiration
Not applicable · inactive patent

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Abstract

A process for synthesizing Gabitril used to prepare the medicines for treating epilepsy and the diseases associated with GABA, its recemate, and its S-configuration are disclosed. Its advantage is low cost.
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Description

technical field

[0001] The invention provides a new synthesis method of Tiagabine, a medicine for treating epilepsy and GABA (γ-Aminobutyric acid) intake-related diseases. The invention also provides the preparation method of racemic tiagabine and S-configuration tiagabine. The invention also provides a preparation method of the optically pure ethyl β-piperidinecarboxylate, which is the raw material needed for synthesizing the above compound. Background technique

[0002]

[0003] In 1991, Nielsen et al. first reported that tiagabine (Tiagabine) had a good antispasmodic effect, and was also a good inhibitor of GABA (γ-Aminobutyric acid) uptake (Eur.J.pharmacol., 1991, 196 (3) , 257-266). At present, it has been developed as a drug for treating epilepsy and GABA (γ-Aminobutyric acid) intake-related diseases (CN 1225094A, 1999, 8, 4). Knud was equal to 1993 and reported its synthetic method (J.Med.Chem., 1993,36,1716-1725), but the two synthetic methods that they used ha...

Claims

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