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Sibutramine aromatic salt of organic acid and its preparation process

An aromatic organic acid, sibutramine hydrochloride technology, applied in the preparation of organic compounds, organic chemistry, chemical instruments and methods, etc., can solve problems such as limited research degree

Inactive Publication Date: 2004-12-29
苏州市玮琪生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although people have achieved certain achievements in these aspects, the degree of research on the formation of salts with better application effects from sibutramine and aromatic organic acids is still very limited.

Method used

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  • Sibutramine aromatic salt of organic acid and its preparation process
  • Sibutramine aromatic salt of organic acid and its preparation process
  • Sibutramine aromatic salt of organic acid and its preparation process

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Embodiment Construction

[0032] The present invention develops and researches a new class of sibutramine aromatic organic acid salts based on predecessors' research results on sibutramine and its salts.

[0033] The invention uses sibutramine hydrochloride as the starting raw material, which is added to the caustic alkali aqueous solution, and the molar ratio of feeding is: hydrochloride: NaOH=1: 1~1: 8, and after a period of reaction, it is extracted with ether. Then dry and concentrate to obtain sibutramine free base as white solid. Then, sibutramine free base and hebenzidine or its derivatives were respectively dissolved in an organic solvent to form a solution, and then the two organic solutions were mixed and stirred at room temperature, and white crystals were precipitated after reacting for 0.5 to 2 hours. , filtered and dried to obtain sibutramine aromatic organic acid salt.

[0034] During the preparation of the free base, the reaction temperature is room temperature, preferably 22°C to 25°C...

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Abstract

The present invention relates to aromatic organic salt of Sibutramine and its preparation process. The hydrochloride of Sibutramine as initial material is added into water solution of caustic alkali and reacted for some time before ethyl ether extraction and drying to concentrate to obtain white solid free Sibutramine alkali. Organic solution of free Sibutramine alkali and organic solution of Haibensaite or its derivative are then mixed at room temperature via stirring to react and separate white crystal, which is dried to obtain the aromatic organic salt of Sibutramine.

Description

technical field [0001] The invention relates to a salt formed by the action of sibutramine and an organic acid, especially a salt formed by the action of sibutramine and a class of aromatic organic acid, and a preparation method of the salt. Background technique [0002] The compound of structure shown in formula I has medical efficacy to organism, according to R 1 , R 2 The difference between the two groups can form a series of compounds. When R 1 , R 2 When both are methyl, it becomes "N,N-dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutylamine", the English name of the compound is "Sibutramine ", the application translates it as "sibutramine", and its structure is shown in formula II. [0003] [0004] British patent specification 2098602 has explained the preparation and application of formula I compound and salt thereof in the treatment of depression; European Patent No. 282206 has explained the application of formula I compound and salt thereof in the trea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C211/26C07C227/16C07C229/38
Inventor 舒亮顾瑜顾善修
Owner 苏州市玮琪生物科技有限公司
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