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Sibutramine aliphatic salt of organic acid, its preparation process and use

A technology of aliphatic organic acids and organic acid salts, applied in organic chemistry and other fields, can solve problems such as limited research

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

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Problems solved by technology

Although people have made certain achievements in these aspects, the degree of research on sibutramine and aliphatic organic acids to form salts with better application effects is still very limited.

Method used

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  • Sibutramine aliphatic salt of organic acid, its preparation process and use
  • Sibutramine aliphatic salt of organic acid, its preparation process and use
  • Sibutramine aliphatic salt of organic acid, its preparation process and use

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Embodiment Construction

[0032] The present invention develops a new type of aliphatic organic acid salt of sibutramine on the basis of previous studies on sibutramine and its salts. The salt can play a more effective role in the prevention and treatment of diseases such as diabetes and obesity. Good results.

[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 pyruvic acid or an aliphatic organic acid similar to pyruvic acid were dissolved in an organic solvent to form a solution, and then the two organic solutions were mixed and stirred at room temperature, and reacted for 0.5 to 2 hours. After that, white crystals are precipitated, filtered and dried to obtain sibutramine aliphatic orga...

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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 ketoacetic acid or similar organic fatty acid are then mixed at room temperature via stirring to react and separate white crystal, which is filtered and dried to obtain the aromatic organic salt of Sibutramine. The salt has excellent diabetes and obesity preventing and treating effect.

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 type of aliphatic organic acid, as well as a preparation method and application 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 s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C211/26C07C229/34
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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