Dextro lipoic amidate and its prepn

A technology of d-lipoic acid and amino acid salt, which is applied in the directions of pharmaceutical formulations, medical preparations containing active ingredients, digestive system, etc., can solve the problems of d-lipoic acid's easy polymerization, thermal stability, insolubility in water, and the like, and achieves good results. Water-soluble, the effect of increasing solubility

Inactive Publication Date: 2007-01-03
GRAND PHARM (CHINA) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So for a long time, how to solve the problems of easy polymerization, poor thermal stability and wat

Method used

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  • Dextro lipoic amidate and its prepn
  • Dextro lipoic amidate and its prepn
  • Dextro lipoic amidate and its prepn

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1: Preparation of D-lipoic acid arginine salt

[0037] raw material name

Feeding amount

mole ratio

D-lipoic acid

L-Arginine

Absolute ethanol

100g

87g

600ml

1

1.05

[0038] operate:

[0039] Put D-lipoic acid, L-arginine, and absolute ethanol into a 1000ml three-necked reaction flask, stir, heat to reflux, and after 2 hours of reflux reaction, evaporate 3 / 4 of the solvent under reduced pressure, and cool the solution at 5-10°C Crystallized, filtered, and dried at 80°C for 6 hours to obtain 172 g of light yellow crystalline solid, yield 94.0%, mp 200-203°C.

Embodiment 2

[0040] Embodiment 2: the preparation of D-lipoic acid lysine salt

[0041] raw material name

Feeding amount

mole ratio

D-lipoic acid

L-Lysine

100g

71g

1

1.0

Ethanol (95%)

600ml

[0042] operate:

[0043] Put D-lipoic acid, L-lysine, and ethanol into a 1000ml three-necked reaction flask, stir, heat to reflux, and after 2 hours of reflux reaction, evaporate 3 / 4 of the solvent under reduced pressure, and cool the solution at 5-10°C to crystallize. After filtration, the crystals were dried at 80°C for 6 hours to obtain 161 g of light yellow crystalline solids, yield 94.2%, mp 195-198°C.

Embodiment 3

[0044] Embodiment 3: Preparation of D-lipoic acid ornithine salt

[0045] raw material name

Feeding amount

mole ratio

D-lipoic acid

Ornithine

Methanol

100g

70g

500ml

1

1.1

[0046] operate:

[0047] Put D-lipoic acid, ornithine, and methanol into a 1000ml three-neck reaction flask, stir, heat to reflux, and after 2 hours of reflux reaction, evaporate 3 / 4 of the solvent under reduced pressure, cool the solution at 5-10°C to crystallize, filter, The crystals were dried at 80°C for 6 hours to obtain 155 g of a light yellow crystalline solid, yield 94.5%, mp 185-187°C.

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PUM

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Abstract

The present invention relates to one kind of medicine, dextro lipoic amidate and its preparation process. The general expression of dextro lipoic amidate is shown. The present invention changes dextro lipoic with easy oxidation and polymerization, poor heat stability and water insolubility into stable dextro lipoic amidate with raised smelting point and raised medicinal effect. The dextro lipoic amidate may be further used to prepare other medicine preparation.

Description

technical field [0001] The invention relates to an amino acid salt used for preparing medicine and a preparation method thereof, in particular to a d-lipoic acid amino acid salt and a preparation method thereof. Background technique [0002] D-lipoic acid (English name R (+) Alpha Lipoic Acid) its molecular formula: C 8 h 14 o 2 S 2 , molecular weight: 206.33, the structural formula is as follows: [0003] [0004] Lipoic acid is an endogenous antioxidant, which can remove free radicals in the body, promote the synthesis of vitamin C by the body using glucose, and promote the synthesis of glutathione, which can effectively remove melanin, and can also assist coenzyme in promoting the body's immunity. Physiological metabolism. Lipoic acid also has anti-inflammatory effects, can inhibit the activity of kinases, transforming factors, d-tumor necrosis factor and collagenase, and has anti-aging effects. Lipoic acid can preserve and regenerate oth...

Claims

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Application Information

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IPC IPC(8): C07D339/04A61K31/381A61P39/06A61P9/00A61P3/10A61P1/16A61P25/28
Inventor 谢国范穆惠芳杨波周建明黄璐
Owner GRAND PHARM (CHINA) CO LTD
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