A kind of semi-synthetic method prepares the production technology of vincamine

A production process and vincamine technology, which is applied in the field of chemical synthesis process, can solve the problems of long route, high production equipment requirements and high cost, and achieve the effects of simple process, safe environment and simple equipment

Active Publication Date: 2016-08-31
ZHANG JIA GANG VINSCE BIO PHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The total synthesis route of vincamine is long, the total yield of these methods is no more than 10%, the cost is too high, and industrial production cannot be realized
[0008] In summary, there are some following problems in the current method of producing vincamine at home and abroad: the total synthesis process route is long, the production enterprise bears high operational risks, and producing a large amount of chemical waste will cause a great burden to the environment, and all of them will affect the production equipment. High requirements, high cost, and low yield
In the semi-synthetic method, difficult-to-handle impurities are easily produced, which need to be removed by column chromatography, which brings inconvenience to industrial production

Method used

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  • A kind of semi-synthetic method prepares the production technology of vincamine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] This example provides a kind of preparation method of vincamine, concrete implementation is as follows:

[0027] 1) Weigh 5.0kg of Tabonin hydrochloride and put it into a 100L stainless steel reactor, add 50L of 75% ethanol, stir at room temperature until Tabonin hydrochloride is completely dissolved, then add 250g of Raney nickel into the reactor, and feed hydrogen , Stir after 0.5h, and control the hydrogen pressure at 1.1atm, and react at room temperature for 8h. After the reaction was completed, nitrogen gas was introduced for 10 minutes, the catalyst Raney nickel was removed by filtration, and the crude product of vinfermin was concentrated to obtain the crude product, which was then crystallized with ethyl acetate-ethanol to obtain 4.8 kg of vinfermin hydrochloride with a purity greater than 99.0%.

[0028] 2) Put the vinformin hydrochloride prepared in step 1) into a 100L stainless steel reaction kettle, add 60L of acetic acid aqueous solution with pH=4.5, stir a...

Embodiment 2

[0031] This example provides a kind of preparation method of vincamine, concrete implementation is as follows:

[0032] 1) Weigh 5.0kg of bonin salt of sulphate and put it into a 100L stainless steel reaction kettle, add 100L of 40% methanol, stir at room temperature until the bonin salt of sulphate is completely dissolved, then add 50g of nickel boride, and pass in hydrogen for 0.5h Stir afterward, and control the hydrogen pressure at 1.1 atm, and react for 12 hours. After the reaction was completed, nitrogen gas was introduced for 10 minutes, the catalyst nickel boride was removed by filtration, concentrated to obtain the crude product of vinbromin, and then crystallized with ethyl acetate-ethanol to obtain 4.0 kg of vinbromin sulfate with a purity greater than 99.0%.

[0033] 2) Put the vinbromin sulfate obtained in step 1) in a 100L stainless steel reaction kettle, add 80L of acetic acid aqueous solution with pH=5, stir and dissolve at room temperature, then fill it with n...

Embodiment 3

[0036] This example provides a kind of preparation method of vincamine, concrete implementation is as follows:

[0037] 1) Weigh 5.0kg of Tabonin hydrochloride and put it into a 100L stainless steel reaction kettle, add 80L of 95% ethanol, stir at room temperature until Tabonin hydrochloride is completely dissolved, then add 500g of PdCO 3, feed hydrogen, stir after 0.5h, and control the hydrogen pressure 1.1atm, react for 8h, after the reaction is completed, feed nitrogen for 10min, filter to remove the catalyst PdCO 3 , concentrated to obtain the crude product of Changchun Fermin, and then crystallized with ethyl acetate-ethanol to obtain 4.6kg of Vinchun Fermin hydrochloride with a purity greater than 99.0%;

[0038] 2) Put the vinbromin hydrochloride obtained in step 1) in a 100L stainless steel reaction kettle, add 50L of acetic acid aqueous solution with pH=4, stir and dissolve at room temperature, then fill with nitrogen protection, and react at room temperature for abo...

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Abstract

The invention discloses a production process using a semi-synthetic method to prepare vincamine. The production process comprises the following steps: using a tabersonine salt as a reaction starting raw material, performing hydrogeneration catalytic reduction, enzyme method hydroxylation and rearranged crystallization to obtain vincamine. The process is simple and short in process route; the obtained vincamine is high in yield and good in purity; the whole production process is low in cost and suitable for industrial production; the enzyme method hydroxylation is performed by oxygenase, so that the process is clean, safe and environment-friendly.

Description

technical field [0001] The present invention relates to the synthetic technology of chemical medicine, specifically a kind of production technology of semi-synthetic method for preparing vincamine. Background technique [0002] Vincamine, the Chinese name is (3α, 4β, 16α)-14,15-dihydro-14-hydroxyivory-14-carboxylate methyl ester, the molecular formula is C 21 h 26 N 2 , which belongs to monoindole alkaloids, is mainly used for the treatment of cerebral ischemia. The clinical indications include cerebrovascular disorders, cerebral embolism, cerebral thrombosis and hemorrhagic sequelae. Because vincamine can penetrate the blood-brain barrier, it has a good effect on dilating blood vessels and increasing cerebral blood flow, but has no effect on the heart, blood vessels and blood pressure. It is a first-line drug for the treatment of cerebral ischemia. [0003] Vincamine was first extracted and isolated from Vinca minor, a plant of the family Apocynaceae. However, the conten...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D461/00
CPCC07D461/00
Inventor 彭学东张梅赵金召闫勇义
Owner ZHANG JIA GANG VINSCE BIO PHARM
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