Method for preparing clofarabine raw material medicament

A raw material drug, the technology of arabinofuranose, applied in the field of medicine, can solve the problems of difficulty, high price, complex synthesis route, etc., and achieve the effect of low manufacturing cost

Inactive Publication Date: 2008-08-13
JILIN PAIGAO BIOLOGICAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The synthetic route of clorabine has been reported. According to the reported synthetic route, it is expected to synthesize clorabine, but the existing synthetic route is relatively complicated, and the ratio of each raw material and the reaction conditions are not accurately determined, and the difficulty of industrial realization is relatively high. Large, the preparation cost is relatively high, and it is not easy to promote in China, which is the main reason why the raw material medicine is not easy to buy in China and the price is relatively expensive

Method used

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  • Method for preparing clofarabine raw material medicament
  • Method for preparing clofarabine raw material medicament
  • Method for preparing clofarabine raw material medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Preparation of Cronabine crude drug, and the synthetic route is shown in Figure 1.

[0028] 1. The instruments used are shown in Table 1:

[0029] Table 1

[0030] Preface

[0031] 7

[0032] 2. Reagents used

[0033] The main raw material specifications and manufacturers are shown in Table 2:

[0034] Table 2:

[0035] raw material name

[0036] Anhydrous magnesium sulfate

[0037] Follow the steps below to prepare Cronabine API:

[0038] (1) Preparation of 1,3,5-3-oxo-benzoyl-α-D-ribofuranose

[0039] Reaction formula:

[0040]

[0041] For ingredients, the weight ratio of 1-oxy-acetyl-2,3,5-tri-oxy-benzoyl-β-D-ribose, dichloromethane, hydrogen bromide, n-hexane and anhydrous magnesium sulfate is 10: 50:1:6:10; or according to the ratio shown in Table 3:

[0042] table 3

[0043] 1-oxy-acetyl-2,3,5-tri-oxy-benzoyl

[0044] Anhydrous magnesium sulfate

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Abstract

The invention discloses a preparing process of clorfarabine raw medicine, specifically provides steps of the process, material ratio and reaction condition of each step. The process is easy to implement, low in cost. The main material 2-chloro inosine is easy to get. The inventive process is beneficial to extensive industrial production of clorfarabine.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a method for preparing a raw material medicine of Cronabine. Background technique [0002] At present, the cure rate of childhood leukemia has increased globally, but the anti-leukemia drugs suitable for children are still blank. The use of adult drugs by children often produces many serious adverse reactions and seriously affects the quality of life of children. [0003] Clofarabine is a nucleotide analogue that combines the advantages of Fludarabine and Cladribine. It inhibits both DNA polymerase and ribonucleic acid reductase. It is currently the only suitable For the treatment of childhood leukemia, studies have shown that its treatment efficiency is very high. The total response rate of patients who did not respond to two conventional chemotherapy to the drug was 31%; and the patients were well tolerated and had no unpredictable adverse reactions. ; Has potential broa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/173
Inventor 梁群欢劳溢权李运南司徒少金董加喜王朝辉
Owner JILIN PAIGAO BIOLOGICAL PHARMA
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