A kind of synthetic method of pterostilbene sodium succinate

A technology of sodium stilbene succinate and a synthesis method, applied in the field of chemical medicine preparation, can solve the problems of unsuitability for large-scale industrial production, long operation time, complicated process and the like, and achieves the advantages of not becoming sticky, easy to operate, and good in reaction yield. Effect

Active Publication Date: 2015-10-21
ZHANG JIA GANG VINSCE BIO PHARM
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  • Abstract
  • Description
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  • Application Information

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Problems solved by technology

Although it has a good slow-release and controlled-release effect, the process is complicated, the process is cumbersome, the operation time is long, the cost is high, and it is uneconomical, so it is not suitable for large-scale industrial production.
[0006] (3) Liposomes and cyclodextrin inclusion compounds also have problems such as complicated procedures, and their finished products have certain biological toxicity

Method used

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  • A kind of synthetic method of pterostilbene sodium succinate

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Experimental program
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Effect test

Embodiment 1

[0022] (1) Esterification reaction: In a 250ml dry three-necked flask, continuously feed N 2 . in N 2 Under protection, 20 g (0.078 mol) of pterostilbene, 10 g (0.1 mol) of succinic anhydride, and 150 ml of tetrahydrofuran were put into the reaction flask. Stir at room temperature until fully mixed and uniform, lower the temperature to 5°C, slowly add 14.4g (0.078mol) of tri-n-butylamine dropwise, after the drop is complete, stir the reaction at a temperature of 5-10°C, and confirm the end point of the reaction by tracking with TLC. After the reaction is completed, control the temperature at 45°C, concentrate under reduced pressure until no solvent is released, add 200ml of dichloromethane and 200ml of 0.1% hydrochloric acid solution for extraction, collect the organic phase, dry it with anhydrous sodium sulfate, concentrate under reduced pressure, and add a small amount of acetone By crystallization, 24.5 g of crude pterostilbene succinate half ester was obtained, with a yi...

Embodiment 2

[0025] (1) Esterification reaction: In a 250ml dry three-necked flask, continuously feed N 2 . in N 2 Under protection, 20 g (0.078 mol) of pterostilbene, 10 g (0.1 mol) of succinic anhydride, and 150 ml of 1,4-dioxane were put into the reaction flask. Stir at room temperature until fully mixed and uniform, lower the temperature to 5°C, slowly add 16.1g (0.078mol) of 1,3-dicyclohexylcarbodiimide dropwise, after the drop is complete, stir the reaction at a temperature of 5-10°C, and the TLC point Plate tracking confirms reaction endpoints. After the reaction is completed, control the temperature at 45°C, concentrate under reduced pressure until no solvent is released, add 200ml of dichloromethane and 200ml of 0.1% hydrochloric acid solution for extraction, collect the organic phase, dry it with anhydrous sodium sulfate, concentrate under reduced pressure, and add a small amount of acetone By crystallization, 20.5 g of crude pterostilbene succinate half ester was obtained, wi...

Embodiment 3

[0028] (1) Esterification reaction: In a 250ml dry three-necked flask, continuously feed N 2 . in N 2 Under protection, 20 g (0.078 mol) of pterostilbene, 10 g (0.1 mol) of succinic anhydride, and 150 ml of tetrahydrofuran were put into the reaction flask. Stir at room temperature until fully mixed evenly, lower the temperature to 5°C, slowly add 9.5g (0.078mol) of 4-dimethylaminopyridine dropwise, after the drop is complete, stir the reaction at a temperature of 5-10°C, and confirm the end point of the reaction by spotting the TLC plate . After the reaction is completed, control the temperature at 45°C, concentrate under reduced pressure until no solvent is released, add 200ml of dichloromethane and 200ml of 0.1% hydrochloric acid solution for extraction, collect the organic phase, dry it with anhydrous sodium sulfate, concentrate under reduced pressure, and add a small amount of acetone By crystallization, 18.4 g of crude pterostilbene succinate half ester was obtained, w...

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Abstract

The invention relates to a synthetic method of pterostilbene sodium succinate which is a pharmaceutical precursor bulk drug. Pterostilbene is used as a raw material, pterostilbene sodium succinate crystals are obtained through an esterification reaction and a salt forming reaction. The process has the advantages that routes are simple, conditions are mild, energy consumption is low and the method is suitable for industrial production and the like, and has high yield, high product content, and good water solubility.

Description

technical field [0001] The invention relates to a synthesis method of pterostilbene sodium succinate, belonging to the technical field of chemical medicine preparation. Background technique [0002] Pterostilbene (Pterostilbene), also known as pterostilbene, chemical name 3,5-dimethoxy-4'-hydroxystilbene, CAS NO.537-42-8, molecular formula C 16 h 16 o 3 , the molecular weight is 256.30. Off-white crystalline powder, insoluble in water, soluble in ethanol, sensitive to air, melting point is 89-92°C. Pterostilbene is a homologue of resveratrol, which has a trans-stilbene skeleton structure. It is an important active ingredient in grapes, blueberries, dried blood products and Indian anti-diabetic herbal medicine "Bijasar". It also exists in Chinese herbal medicine, and its pharmacological effects are partially similar to those of resveratrol. It is a good antioxidant and has many activities such as anti-inflammation, anti-thrombosis, anti-cancer, anti-cancer, and anti-hyper...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C69/40C07C67/00C07C67/08
Inventor 彭学东张梅赵金召弓旻
Owner ZHANG JIA GANG VINSCE BIO PHARM
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