Method for preparing dasatinib tablets

A technology of dasatinib and quantitative ratio, which is applied in the field of drug synthesis, can solve the problems of long synthetic routes, impure intermediate products, and large environmental pollution, and achieve the effects of increased yield, short reaction time, and reduced pollution
CN109503568AActive Publication Date: 2019-03-22SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD +2
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
Publication Date
2019-03-22

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Abstract

The invention relates to a method for preparing dasatinib tablets. The method comprises the following steps: enabling 3-oxo-ethyl propionate to react with 2-chlorine-6-methylaniline under an alkali condition, further adding a solvent in which cupric bromide is dissolved to carry out a reaction, further adding thiourea, and cyclizing with a catalyst so as to obtain 2-amino-N-(2-chlorine-6-methyphenyl)thiazole-5-formamide; further synthesizing dasatinib tablets from 4,6-dichloro-2-methyl pyrimidine, N-ethoxy piperazine and 2-amino-N-(2-chlorine-6-methyphenyl)thiazole-5-formamide according to a one-pot method under the action of an alkali and an ionic liquid 1-butyl-3-methylimidazole glycinate. The method is mild in condition, simple in step, environmentally friendly, high in yield and applicable to industrial production.
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Description

technical field

[0001] The invention relates to the field of drug synthesis, in particular to a preparation method of dasatinib. Background technique

[0002] Dasatinib (Dasatinib, trade name Sprycel), chemical name N-(2-chloro-6-methylphenyl)-2-[6-[4-(2-hydroxyethyl)-1-piper Azinyl]-2-methyl-4-pyrimidinyl]amino-5-thiazole carboxamide is an oral tyrosine kinase inhibitor developed by Bristol-Myers Squibb. The drug was approved by the FDA in June 2006 for the treatment of chronic myelogenous leukemia and also for the treatment of Philadelphia chromosome-positive acute lymphoblastic leukemia. This product has inhibitory effects on various mutants of Bcr-Ab1 kinase, and the inhibitory intensity is much higher than that of Imatinib, and no drug resistance has been found. Its structural formula is as follows:

[0003]

[0004] Regarding the synthesis of dasatinib, there are many domestic and foreign literature reports, most of which are intermediate 2-amino-N-(2-chloro-6-me...

Claims

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