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Vincristine and method for synthesizing vincristine sulfate

A technology of vincristine and synthetic methods, applied in the direction of organic chemistry, etc., can solve the problems of complex process steps and high production costs, and achieve the effects of simple process, low production cost and cost reduction

Inactive Publication Date: 2014-08-06
HUBEI HONCH PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The method adopts a two-step synthesis method to synthesize vincristine, the process steps are complicated, and the production cost is high

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Weigh 100g of vinblastine sulfate and add it to 500mL of purified water. After it is completely dissolved, add 16.5mL of ammonia to adjust the pH of the solution to 7.5, and then add enough dichloromethane for extraction. After layering, remove the supernatant. The lower organic phase was concentrated with a rotary evaporator, spin-dried, and then drained with a vacuum oil pump to obtain 85 g of light yellow powder vinblastine.

[0041] Weigh 50g of vinblastine and add it to 2500mL of tetrahydrofuran to prepare a vinblastine solution with a concentration of 0.02g / mL, then place the vinblastine tetrahydrofuran solution in a low temperature and constant temperature reaction bath, and add 187.5 dropwise to the vinblastine solution mL acetic acid, when the temperature of the low-temperature thermostatic reaction bath drops to -65°C, keep it warm, drop 445 mL of sodium dichromate solution with a concentration of 0.18 g / mL at a rate of 12 mL / min, and continue the reaction for 2 h...

Embodiment 2

[0049] Weigh 100 g of vinblastine sulfate and add it to 380 mL of purified water. After it is completely dissolved, add 18 mL of ammonia to adjust the pH of the solution to 8, and then add sufficient dichloromethane for extraction. After layering, remove the supernatant The lower organic phase was concentrated with a rotary evaporator, spin-dried, and then drained with a vacuum oil pump to obtain 81 g of light yellow powder vinblastine.

[0050] Weigh 50g of vinblastine and add it to 2000mL of tetrahydrofuran to prepare a vinblastine solution with a concentration of 0.025g / mL, then place the vinblastine tetrahydrofuran solution in a low temperature and constant temperature reaction bath, and add 187.5 dropwise to the vinblastine solution mL acetic acid, when the temperature of the low-temperature thermostatic reaction bath drops to -63°C, keep it warm, drop 445 mL of sodium dichromate solution with a concentration of 0.18 g / mL at a rate of 14 mL / min, and continue the reaction for ...

Embodiment 3

[0058] Weigh 100 g of vinblastine sulfate and add it to 450 mL of purified water. After it is completely dissolved, add 16 mL of ammonia to adjust the pH of the solution to 8.0, and then add enough dichloromethane for extraction. After layering, remove the supernatant The lower organic phase was concentrated with a rotary evaporator, spin-dried, and then drained with a vacuum oil pump to obtain 82.6 g of light yellow powder vinblastine.

[0059] Weigh 50g of vinblastine and add it to 2250mL of tetrahydrofuran to prepare a vinblastine solution with a concentration of 0.022g / mL, then place the vinblastine tetrahydrofuran solution in a low temperature and constant temperature reaction bath, and add 187.5 dropwise to the vinblastine solution mL of acetic acid, when the temperature of the low-temperature thermostatic reaction bath drops to -67℃, keep it warm, and add 445 mL of sodium dichromate solution with a concentration of 0.18 g / mL at a rate of 12 mL / min. After the addition, conti...

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Abstract

The invention discloses vincristine and a method for synthesizing vincristine sulfate. The method for synthesizing vincristine comprises the following steps: 1) preparing vinblastine; and 2) synthesizing, purifying and refining vincristine, namely carrying out reaction on the synthesized vincristine and ethanol sulfate on the basis of the method for synthesizing vincristine, so as to obtain a crude product of the vincristine sulfate, and refining the crude product of the vincristine sulfate to obtain the vincristine sulfate. The vincristine is synthesized by adopting a one-step synthesis method when the vincristine is synthesized, the synthetic route of the vincristine is simplified, the method is simple in synthetic route, and low in production cost, the purity of the synthesized vincristine can be up to over 96% after the synthesized vincristine is refined, and the vincristine sulfate is synthesized on the basis of the method for synthesizing the vincristine. The process for synthesizing the vincristine is simple, so that the synthetic route of the vincristine sulfate is greatly simplified, the method is simple in synthetic route, and low in production cost, and the purity of the refined vincristine sulfate can be up to over 96%.

Description

Technical field [0001] The invention relates to a synthesis method of vincristine and vincristine sulfate, and belongs to the technical field of alkaloid preparations. technical background [0002] Vincristine is an indole compound. Its chemical structure is a fused four-membered ring containing an indole nucleus and another fused five-membered ring containing an indole nucleus directly connected by carbon-carbon bonds, totaling 9 Asymmetric centers. Vincristine has the effect of stopping cell division (mitosis) in the middle stage. Like colchicine, it can bind to tubulin to inhibit its biological activity, but the binding site is different and the effect is stronger than that of colchicine. The difference between vincristine and colchicine is that it also acts on proteins other than tubulin, such as actin and 10 nanometer fibrin. It is especially effective for tumors in hematopoietic organs. Vincristine is used in clinical medicine. One of the anticancer agents is used. Vincr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D519/04
CPCC07D519/04
Inventor 张文凯何福彪何绍春
Owner HUBEI HONCH PHARMA
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