Method for preparing furanone compounds

A compound, the technology of furanone, which is applied in the field of preparation of furanone compounds, can solve the problems of low product purity, low total yield, cumbersome post-processing steps, etc.
CN106588831AActive Publication Date: 2017-04-26上海云晟研新生物科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
上海云晟研新生物科技有限公司
Publication Date
2017-04-26

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Abstract

The invention discloses a method for preparing furanone compounds, and provides a method for preparing a furanone compound III. The method includes the following steps that in a solvent, in the presence of inorganic salt, a compound II and a reducing agent are subjected to a reduction reaction, and the furanone compound III is obtained; the solvent is a fatty alcohol solvent or a mixed solvent of a fatty alcohol solvent and water. The brivaracetam can be prepared with the furanone compound III only with the three steps, and the synthetic route is short; the ee value of the compound II is larger than 99.0%, racemization does not occur in the reaction process, and the de value of a brivaracetam I crude product is larger than 99.0%; the brivaracetam I crude product is further purified through a crystal instead of a chirality high-pressure-liquid-phase preparing column, and the chirality purity of brivaracetam I can be further increased to be the de value of 99.80% or above; meanwhile, the content of other individual impurities of the brivaracetam I is smaller than 0.1%, and reaches the API level, and the method is suitable for industrial production. The formula is defined in the description.
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Description

technical field

[0001] The present invention relates to a preparation method of furanone compounds. Background technique

[0002] Brivaracetam I is a racetam derivative with broad antiepileptic activity and high safety profile. Belgian pharmaceutical giant UCB (UCB) has published data from a 12-week phase III study of the epilepsy drug brivaracetam, which showed that brivaracetam significantly reduced the frequency of partial seizures and improved response rates. The tolerability of brivaracetam in the study was consistent with previous studies. UCB submitted the New Drug Application and Marketing Authorization Application for brivaracetam to the FDA and the European Medicines Agency (EMA) respectively in 2015 and has been approved, making brivaracetam the third of UCB's flagship epilepsy franchise Marketed product, the company is conducting late-stage studies seeking approval for the drug in pediatric patients, as well as as a monotherapy in adult patients.

[0003] ...

Claims

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