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Synthetic method of alpha-lipoic acid zinc

A synthesis method and technology of zinc lipoate, applied in the direction of organic chemistry and the like, can solve problems such as complicated procedures and long process cycle, and achieve the effects of simple process, low environmental toxicity and good reaction yield

Inactive Publication Date: 2014-06-25
ZHANG JIA GANG VINSCE BIO PHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] As a biological drug, zinc lipoate has good biocompatibility and has attracted strong attention from the medical community. Chinese patents CN200510081700.9 and CN200610009181.X respectively introduce R-lipoic acid zinc and R-(+)-lipoic acid The synthesis method of zinc, but its procedure is relatively loaded down with trivial details, and process cycle is longer

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Add 17.8g of α-lipoic acid and 200ml of methanol into a 500mL glass three-necked flask, start stirring, add dropwise 3ml of 80% sodium hydroxide aqueous solution, the dropwise addition is complete, add 13g of zinc chloride while stirring, concentrate under reduced pressure, and remove 80% of the solvent , the precipitate was collected, washed with water, and dried in vacuum to obtain the product. Yield 88.9%, purity 98.6% (HPLC).

Embodiment 2

[0019] Add 17.8g of α-lipoic acid and 200ml of ethanol into a 500mL glass three-necked flask, start stirring, add 6ml of 40% sodium hydroxide aqueous solution dropwise, the dropwise addition is complete, add 15.5g of zinc sulfate while stirring, concentrate under reduced pressure, and remove 80% of the solvent , the precipitate was collected, washed with water, and dried in vacuum to obtain the product. Yield 88.3%, purity 98.6% (HPLC).

Embodiment 3

[0021] Add 17.8g of α-lipoic acid and 200ml of methanol into a 500mL glass three-necked flask, start stirring, add dropwise 6ml of 59% potassium hydroxide aqueous solution, the dropwise addition is complete, add 12.7g of zinc nitrate while stirring, concentrate under reduced pressure, and remove 80% of the solvent , the precipitate was collected, washed with water, and dried in vacuum to obtain the product. Yield 88.5%, purity 98.7% (HPLC).

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Abstract

The invention relates to a synthetic method of an organic drug alpha-lipoic acid zinc. Specifically, the synthetic method comprises: by taking alpha-lipoic acid as the raw material, preparing the alpha-lipoic acid into the alpha-lipoic acid zinc by virtue of one-step salt forming reaction. The synthetic method is simple, easy to implement, low in toxicity, environment-friendly, high in yield and high in content of product.

Description

technical field [0001] The invention relates to the field of medicinal organic chemistry, in particular to a method for synthesizing alpha-lipoic acid zinc. Background technique [0002] α-Lipoic Acid (α-Lipoic Acid), Molecular Formula C 8 h 14 o 2 S 2 , referred to as α-LA, is a water-soluble and fat-soluble metabolic antioxidant, a vitamin-like substance. Its isomer, R-lipoic acid, is a natural substance that widely exists in animal and plant cells. It is a coenzyme that oxidizes and decarboxylates α-ketocarboxylic acids, and can also make vitamin C, vitamin E, and glutathione and coenzyme Q10 regenerating antioxidants. Lipoic acid racemate is useful in the treatment of hepatic lesions and neuropathies, in addition to possessing cytoprotective anti-inflammatory and analgesic activities. [0003] With the in-depth study of the pharmacology and pharmacodynamics of lipoic acid, it was found that lipoic acid has poor thermal stability, easy to polymerize under aerobic co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D339/04
CPCC07D339/04
Inventor 彭学东张梅赵金召弓旻
Owner ZHANG JIA GANG VINSCE BIO PHARM
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