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A kind of semi-synthetic production method of vinpocetine

A technology of vinpocetine and a production method, which is applied in the field of semi-synthetic production of vinpocetine, can solve the problems of poor safety, low yield and low quality, and achieves the effects of increasing safety, simple process route and simplifying purification process

Active Publication Date: 2016-05-04
广州普星药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Above-mentioned two kinds of processing routes, in actual production, all there are many problems, and safety is relatively poor, as all need to adopt pressurized catalysis; The oxidizing agent of use, as m-chloroperoxybenzoic acid, p-nitroperoxybenzoic acid are all Vitiligo drug, high-concentration hydrogen peroxide such as 50%, 60%, 90%, all have certain danger in the process of its storage, transportation and use; Gained vincamine crude product, quality is low, need through loaded down with trivial details aftertreatment, such as Multi-step column chromatography and recrystallization, etc., can obtain high-purity products, but the yield is also very low, resulting in high cost

Method used

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  • A kind of semi-synthetic production method of vinpocetine
  • A kind of semi-synthetic production method of vinpocetine
  • A kind of semi-synthetic production method of vinpocetine

Examples

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Effect test

Embodiment 1

[0051] A kind of semi-synthetic production method of vinpocetine, concrete steps are as follows:

[0052] 1) Preparation of Tabonin Hydrogenate Hydrochloride:

[0053] In a 100L enamel reaction kettle, add 41kg of 90% ethanol, start stirring, then add 5kg (13.41mol) of bonin hydrochloride (purity: 91.15%), and quickly add 0.5kg of 10% new Pd / C. Seal the lid of the kettle, replace it with nitrogen three times, then replace it with hydrogen (purity: 99.999%) three times, pass hydrogen at normal temperature and pressure, stir rapidly, and react for 10 hours, take a sample from the sampling hole, and spot the plate with TLC Analyze until there is no raw material it bonin hydrochloride. After the reaction is over, filter and recycle Pd / C, and wash the filter cake with 0.5kg of ethanol, collect and seal the Pd / C, with a wet weight of 0.80kg, and place the mother liquor at 60°C, - Under 0.09~-0.098MPa, distill under reduced pressure, collect distillate ethanol and water, obtain 4.8...

Embodiment 2

[0066] A kind of semi-synthetic production method of vinpocetine, concrete steps are as follows:

[0067] 1) Preparation of Tabonin Hydrogenate Hydrochloride:

[0068] In a 100L enamel reaction kettle, add 41kg (50L) of process ethanol, start stirring, add 5kg (13.41mol) of bonin hydrochloride (purity 98%), quickly add 0.4kg of 10% new Pd / C , then add wet weight 0.8kg in Example 1 to collect and seal the reclaimed Pd / C, seal the lid of the kettle, replace it with nitrogen three times, and then replace it three times with hydrogen (purity: 99.999%), and pass hydrogen at normal temperature and pressure After 10 hours of reaction, take a sample from the sampling hole and analyze it with TLC until the reaction of bonin hydrochloride is complete; after the reaction, filter and recover Pd / C, wash the filter cake with 0.5kg of ethanol, collect and seal it well Pd / C, wet weight 0.80kg, distill the mother liquor at 60°C, -0.09~-0.098MPa under reduced pressure, collect distillate ethan...

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Abstract

The invention discloses a semisynthetic production method of vinpocetine, a tabersonine hydrochloride is used as a raw material, Pd / C is used as a catalyst, tabersonine hydrogenation hydrochloride is obtained under normal temperature and pressure, monoperoxy maleic acid is prepared by use of hydrogen peroxide, vincamine is prepared by oxidation, reduction, transposition, settlement and washing then, and the vincamine is hydrolyzed, dehydrated and converted into vinpocetine. The semisynthetic production method of vinpocetine is simple in operation and high in safety, increases the yield, and reduces production cost, and a high purity product can be obtained without column chromatography.

Description

technical field [0001] The invention relates to the technical field of organic synthesis, in particular to a semi-synthetic production method of vinpocetine. Background technique [0002] Vinpocetine is a natural medicine originally obtained from periwinkle, which belongs to indole alkaloids, and is mainly used to improve various symptoms induced by cerebral infarction sequelae, cerebral hemorrhage sequelae, and cerebral arteriosclerosis. Vinpocetine for injection is a cerebral vasodilator, which can inhibit the activity of phosphodiesterase, increase the effect of c-GMP, the messenger of vascular smooth muscle relaxation, and selectively increase cerebral blood flow. In addition, it can also inhibit platelet aggregation and reduce human blood viscosity. , enhance the deformability of red blood cells, improve blood flow and microcirculation, promote glucose uptake by brain tissue, increase brain oxygen consumption, and improve brain metabolism. [0003] The English name of ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D461/00
CPCC07D461/00
Inventor 朱义波邓团飞冯正喜陈秀秀
Owner 广州普星药业有限公司