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Method for semisynthesis of vincristine sulfate

A technology of vincristine sulfate and vinblastine sulfate, which is applied in the field of semi-synthetic vincristine sulfate, can solve the problems of unfeasible production, low reaction conversion rate, complicated post-processing, etc., and achieves remarkable economic value and high yield , Environmentally friendly effect

Inactive Publication Date: 2018-04-06
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

The reaction conversion rate of this method is low, the post-treatment is complicated, and multiple refinements are required after the salt is formed, so that the yield is very low, resulting in a very high cost, and the production is not feasible.

Method used

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  • Method for semisynthesis of vincristine sulfate
  • Method for semisynthesis of vincristine sulfate

Examples

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Comparison scheme
Effect test

Embodiment 1

[0053] A method for semi-synthesizing vincristine sulfate, comprising the following steps:

[0054] 1. Refining of crude vinblastine sulfate:

[0055] Weigh 420mL of purified water, add it to a 3L Erlenmeyer flask, and heat to 60-70°C; weigh 210g of crude vinblastine sulfate, add it to the above hot water, dissolve it, and quickly add it to 5040mL of In the water ethanol, a large amount of solids precipitated. After stirring evenly, keep it airtight at room temperature for 1 day; after rapid filtration, wash the filter cake with a small amount of cold absolute ethanol for 2 to 3 times, drain it, and spread it on the Put it in a drying oven tray, put it in a vacuum drying oven, and dry it under reduced pressure (-0.08~-0.1MPa) at 50-60°C for 4 hours to obtain the primary crystallization product of vinblastine sulfate; in the same way, recrystallize the primary crystallization product of vinblastine sulfate Once, refined vinblastine sulfate: 180g (hereinafter referred to as: in...

Embodiment 2

[0069] A method for semi-synthesizing vincristine sulfate, comprising the following steps:

[0070] 1. Refining of crude vinblastine sulfate:

[0071] Weigh 420mL of purified water, add it to a 3L Erlenmeyer flask, and heat to 60-70°C; weigh 210g of crude vinblastine sulfate, add it to the above hot water, dissolve it, and quickly add it to 5040mL of In the water ethanol, a large amount of solids precipitated. After stirring evenly, keep it airtight at room temperature for 1 day; after rapid filtration, wash the filter cake with a small amount of cold absolute ethanol for 2 to 3 times, drain it, and spread it on the Put it in a drying oven tray, put it in a vacuum drying oven, and dry it under reduced pressure (-0.08~-0.1MPa) at 50-60°C for 4 hours to obtain the primary crystallization product of vinblastine sulfate; in the same way, recrystallize the primary crystallization product of vinblastine sulfate Once, refined vinblastine sulfate: 179g (hereinafter referred to as: in...

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Abstract

The invention discloses a method for semisynthesis of vincristine sulfate. The method comprises the following steps: taking a vinblastine sulfate crude product as a raw material, firstly refining to obtain high purity, carrying out oxidation and formylation to generate a vincristine crude product, purifying through alumina column chromatography, and directly salifying, so that the vincristine sulfate is obtained. The method disclosed by the invention is simple in technological operation and easy in aftertreatment, a salifying product can obtain the purity reaching higher than 97% without refining, yield reaches 40-50%, and cost is greatly reduced, so that the method disclosed by the invention has production feasibility and high economic value.

Description

technical field [0001] The invention relates to the technical field of chemical synthesis, in particular to a method for semi-synthesizing vincristine sulfate. Background technique [0002] The English name of vincristine sulfate is Vincristine Sulphate, CAS NO: 2068-78-2, and the molecular formula is C 46 h 56 N 4 o 10 ·H 2 SO 4 , the molecular weight is 923.04, and the structural formula is as follows: [0003] [0004] Vincristine is a bis-indole alkaloid compound, and its target is microtubules, mainly inhibiting the polymerization of tubulin and affecting the formation of spindle microtubules, so that mitosis stops in metaphase. It can also interfere with protein metabolism and inhibit the activity of RNA polymerase, and inhibit the synthesis of cell membrane lipids and the transport of amino acids on the cell membrane. The inhibitory effect of vincristine on transplanted tumors is greater than that of vinblastine and has a broad antitumor spectrum, especially...

Claims

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Application Information

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IPC IPC(8): C07D519/04
CPCC07D519/04
Inventor 邓团飞唐星王小力王亚峰
Owner 广州普星药业有限公司
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