A kind of synthetic method of vinblastine sulfate

Abstract

The invention discloses a preparation method of vinblastine sulfate, comprising: 1) the preparation step of dehydrated vinblastine reaction solution: taking pendolin or its corresponding salt, vinblastine or its corresponding salt as raw materials, Reaction under the action of ferric chloride to obtain dehydrated vinblastine reaction liquid; 2) preparation steps of vinblastine crude product: add in the mixed solution of iron oxalate and water in the dehydrated vinblastine reaction liquid, feed air, add boron dropwise Sodium hydride is carried out reduction reaction, obtains vinblastine crude product; 3) the purification step of vinblastine crude product: vinblastine crude product is purified by column, obtains vinblastine pure product; 4) the preparation step of vinblastine sulfate: vinblastine pure product is carried out with sulfuric acid Salt-forming reaction to obtain vinblastine sulfate. The raw material of the invention is cheap and easy to obtain, does not need refining, simplifies the technological process, has few reaction by-products, high product yield and high purity, and is suitable for large-scale production.

Description

A kind of synthetic method of vinblastine sulfate technical field The present invention relates to chemical synthesis technical field, be specifically related to a kind of synthetic method of vinblastine sulfate. Background technique Vinblastine sulfate English name VinblastineSulfate, CASNo.143-67-9, molecular formula C 46 H 58 N 4 O 9 · H 2 SO 4 , the molecular weight is 909.06, and the structural formula is as follows: [0003] [0004] Vinblastine sulfate mainly inhibits the polymerization of tubulin, but hinders the formation of spindle microtubules and stops mitosis. end in the mid-term. It can also act on the cell membrane, interfere with the transport of amino acids by the cell membrane, inhibit protein synthesis, and also inhibit RNA synthesis. Mainly used for the treatment of solid tumors. It has good curative effect on malignant lymphoma, testicular tumor and choriocarcinoma, and has good effect on lung cancer, Breast cancer, ova...

AI Technical Summary

Problems solved by technology

But there are obvious deficiencies in the technology of plant extraction, such as the low content of vinblastine in periwinkle, and the extraction yield is not high, one ton of periwinkle can only extract several grams of high-purity vinblastine, and then the extraction process and its refining The process requires a large amount of organic solvents, and a large amount of periwinkle waste needs to be treated after extraction, and a large amount of waste water is generated, which is not friendly to the environment

[0007] 2. Biotechnology preparation: There are few researches on the biosynthesis process at present, limited by its low yield, high workshop, equipment and production costs, and it is currently difficult to scale production

The raw material dehydrated vinblastine used in this patent is also in short supply. In addition, the content of vinblastine sulfate obtained is relatively low, which is difficult to meet the quality requirements of the market.

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