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Industrial production process for indole alkaloid tabersonine

A technology of taponin and alkaloids, applied in the industrial production process of indole alkaloids-taponin, can solve the problems of high cost, high energy consumption, large pollution, etc., and achieve the effect of good extraction recovery rate

Inactive Publication Date: 2012-07-04
江苏斯威森生物医药工程研究中心有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0011] The present invention needs to solve the disadvantages of low extraction recovery rate, heavy pollution, high energy consumption and high cost in the prior art, and aims to establish a high-efficiency, low-cost An industrialized process route for the production of bonin alkaloids from Voacanga africana fruit seeds, which is concise and high recovery rate

Method used

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  • Industrial production process for indole alkaloid tabersonine
  • Industrial production process for indole alkaloid tabersonine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1 The preparation method 1 of Tabonin alkaloid

[0025] Get Voacanga africana fruit seeds with a moisture content of less than 2%, pulverize and pass through a 60-mesh sieve. Weigh 1 kg of Voacanga africana fruit seed powder, soak in 3 L of sodium hydroxide solution with a pH value of 9, and ultrasonically disrupt cell tissue for 1 h. Filter and dry to obtain Voacanga africana fruit seed powder, and recover and recycle the lye. Put the dried Voacanga africana fruit seed powder in a multi-functional extraction tank, and extract it twice with 6L industrial methanol, each time for 4h (the recovery rate of the bonin alkaloid extraction detected by HPLC should be greater than 98%, otherwise, extract it with 6L methanol 2h, filtered methanol (applicable), filtered and concentrated to obtain Voacanga africana fruit seed methanol extraction fluid extract, methanol recovery and recycling. Disperse the liquid extract above in 3L of water, adjust the pH value to 3.0 w...

Embodiment 2

[0026] Embodiment 2 The preparation method of Tabonin alkaloid 2

[0027] Get Voacanga africana fruit seeds with a moisture content of less than 2%, pulverize and pass through a 60-mesh sieve. Weigh 1 kg of Voacanga africana fruit seed powder, soak in 3 L of ammonia solution with a pH value of 9, and ultrasonically disrupt cell tissue for 1 h. Filter and dry to obtain Voacanga africana fruit seed powder, and recover and recycle the lye. Put the dried Voacanga africana fruit seed powder in a multi-functional extraction tank, and extract it twice with 6L industrial methanol, each time for 4h (the recovery rate of the bonin alkaloid extraction detected by HPLC should be greater than 98%, otherwise, extract it with 6L methanol 2h, filtered methanol (applicable), filtered and concentrated to obtain Voacanga africana fruit seed methanol extraction fluid extract, methanol recovery and recycling. Disperse the above liquid extract in 3L of water, adjust the pH value to 3.0 with dilut...

Embodiment 3

[0028] Embodiment 3 Itbonin hydrochloride preparation method 1

[0029] Heat and dissolve 24.0 g of oily Tabonin alkaloid in 500 mL of anhydrous methanol, then adjust the pH value to 3.0 with concentrated hydrochloric acid, then pump out about 200 mL of methanol under reduced pressure, and cool to precipitate Tabonin coarse crystals. Then recrystallized from methanol to obtain 23.0 g of refined Tabonin hydrochloride. HPLC detection content is greater than 99.5%.

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Abstract

The invention discloses an industrial production process for indole alkaloid tabersonine. The tabersonine is an important raw material for synthesizing series of cerebral ischemia and senile dementia resistant medicines, namely vincamine, vinpocetine and vinburnine. According to the method, the tabersonine is prepared by steps of soaking in a basic solution, breaking cell tissues by using ultrasonic waves for extraction, extracting and separating at a specific pH value, and purifying in a special solution. The tabersonine with the purity of over 99.0 percent prepared by the method has the recovery rate of over 92 percent and the process is suitable for industrially producing the tabersonine.

Description

technical field [0001] The invention relates to an industrialized production process of an indole alkaloid - tabonin. It is a key raw material for synthesizing series of anti-cerebral ischemia and senile dementia drugs vincamine, vinpocetine and vincabutin, and it also has certain antihypertensive pharmacological activity. This method uses lye immersion, advanced ultrasonic tissue cell crushing and extraction, specific pH value extraction and separation and special solvents to prepare pure Tabonin salt. Compared with previous domestic and foreign reports, this process greatly improves the purity and quality of Tabonin. Recovery rate. Background technique [0002] Tabersonine (Tabersonine) is an indole alkaloid, which itself has a small antihypertensive activity. It is a key raw material for the synthesis of first-line anti-cerebral ischemia and senile dementia drugs vincamine, vinpocetine and vinpobutynin, and is very important. Drug synthesis intermediates. The compound ...

Claims

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Application Information

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IPC IPC(8): C07D471/20
Inventor 彭学东王正濂龚福春张梅
Owner 江苏斯威森生物医药工程研究中心有限公司
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