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Vincamine preparation method

A vincamine and a certain amount of technology, applied in the field of compound preparation, can solve the problems of large amount of catalytic hydrogenation catalyst, high oxidant risk, and difficulty in obtaining raw materials, and achieve the effects of improved yield, easy recovery and application, and easy purchase.

Active Publication Date: 2017-05-31
NORTHEAST PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] The purpose of the present invention is to provide a kind of preparation method of vincamine, to solve the problem that existing catalytic hydrogenation catalyst consumption is large, it is easy to burn when exposed to the air, the danger of preparing oxidant is high, the raw material is not easy to obtain, post-reaction treatment is difficult, time-consuming, Problems such as high product isomers

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The impact of using different hydrogenation reaction solvents on the reaction:

[0046] (1) Preparation of Itbonin:

[0047]Add 30.0g (80.4mmol) of bonin hydrochloride and 325.0g of petroleum ether into a 1000mL four-necked bottle, add 12.3g (87.7mmol) of ammonia water dropwise under stirring, stir at 25°C for 0.5h after dropping, and then add 330g of saturated sodium bicarbonate solution was stirred for 0.5h. After the reaction was completed, the layers were separated, and the aqueous layer was extracted twice with 2×65g petroleum ether. The organic phases were combined, dried by adding 5 g of anhydrous magnesium sulfate for 2 h, filtered with suction, and the petroleum ether was distilled off under reduced pressure at 50° C. to obtain 27.0 g of Tabonin with a mass yield of 90%.

[0048] (2) Preparation of Vinca Manfermin

[0049] Add 26.0g (77.3mmol) tabonin in the 1000ml four-necked bottle that is furnished with tee, 208.0g organic solvent dissolves, and described...

Embodiment 2

[0057] The impact of adopting different hydrogenation reaction temperatures on the reaction:

[0058] (1) Preparation of Itbonin:

[0059] Add 30.0g (80.4mmol) of bonin hydrochloride and 325.0g of petroleum ether into a 1000mL four-neck bottle, add 12.3g (87.7mmol) of ammonia water dropwise under stirring, stir at room temperature for 0.5h after dropping, and then add 330g Saturated sodium bicarbonate solution was stirred for 0.5h. After the reaction was completed, the layers were separated, and the aqueous layer was extracted twice with 2×65g petroleum ether. The organic phases were combined, dried by adding 5 g of anhydrous magnesium sulfate for 2 h, filtered with suction, and the petroleum ether was distilled off under reduced pressure at 50° C. to obtain 27.0 g of Tabonin with a mass yield of 90%.

[0060] (2) Preparation of Vinca Manfermin

[0061] Add 26.0g (77.3mmol) Tabonin to a 1000ml four-necked bottle equipped with a tee, dissolve in 208.0g methanol, add 2.6g Pd / ...

Embodiment 3

[0069] The influence of different oxidation reaction oxidant additions on the reaction:

[0070] (1) Preparation of Itbonin:

[0071] Add 30.0g (80.4mmol) of bonin hydrochloride and 325.0g of petroleum ether into a 1000mL four-neck bottle, add 12.3g (87.7mmol) of ammonia water dropwise under stirring, stir at room temperature for 0.5h after dropping, and then add 330g Saturated sodium bicarbonate solution was stirred for 0.5h. After the reaction was completed, the layers were separated, and the aqueous layer was extracted twice with 2×65g petroleum ether. The organic phases were combined, dried by adding 5 g of anhydrous magnesium sulfate for 2 h, filtered with suction, and the petroleum ether was distilled off under reduced pressure at 50° C. to obtain 27.0 g of Tabonin with a mass yield of 90%.

[0072] (2) Preparation of Vinca Manfermin

[0073] Add 26.0g (77.3mmol) Tabonin to a 1000ml four-necked bottle equipped with a tee, dissolve in 208.0g methanol, add 2.6g Pd / C und...

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Abstract

The invention relates to a vincamine preparation method in the field of compound preparation. The vincamine preparation method includes the steps of (1), tabersonine preparation, (2), vincadifformine preparation, (3), monoperoxy maleic acid preparation and (4), vincamine preparation. The vincamine preparation method has the advantages of easy availability to raw materials, simplicity and convenience in reaction process operation, high safety, low cost, high product yield, high quality and suitability for industrial production.

Description

technical field [0001] The invention relates to a preparation method of Vincamine in the field of compound preparation. Background technique [0002] Vinpocetine is a structurally modified derivative of the alkaloid vincamine, and is an excellent drug for treating cerebrovascular diseases. It is highly fat-soluble and easily enters the brain tissue through the blood-brain barrier. It is widely used in the treatment and prevention of ischemic cerebrovascular diseases. Clinically, it has been widely used in ischemic cerebrovascular disease, hemorrhagic cerebrovascular disease, vascular dementia, vertebral-basilar artery insufficiency, vertigo, depression, traumatic subdural effusion, memory impairment, cognitive dysfunction, Cerebellar atrophy, migraine, visual system disease, auditory system disease and lower extremity atherosclerosis. Vinpocetine has attracted the attention of domestic and foreign experts because of its good clinical efficacy and unique pharmacological eff...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D461/00
CPCC07B2200/07C07D461/00
Inventor 李洋张卫军刘素娜白洁陶芳邸矾董爱军杨璐李冶王龙韩晓丹
Owner NORTHEAST PHARMA GRP
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