Preparation technology o high-purity gefitinib

A gefitinib and preparation process technology, applied in the field of pharmaceutical compound preparation, can solve the problems of many types of solvents, long production cycle, many steps, etc., and achieve the effects of high purity, reduced production cost, and reduced types

CN102584720AActive Publication Date: 2012-07-18REYOUNG PHARMA

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Patent Information

Authority / Receiving Office: CN · China
Patent Type: Applications(China)
Current Assignee / Owner: REYOUNG PHARMA
Publication Date: 2012-07-18

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Abstract

The invention relates to the preparation technology of high-purity gefitinib and belongs to the technical field of preparation of medical compounds. The technology is characterized in that 4-chlorine-7-methoxyl -6-(3-morpholin-4-ylpropoxy) quinazoline hydrochloride and 3-chlorine-4-fluoroaniline are in direct reaction, so as to obtain gefitinib hydrochloride, then gefitinib crude products can be obtained through neutralization, and finally, the high-purity gefitinib is obtained by post processing. In the invention, the the 4-chlorine-7-methoxyl-6-(3-morpholin-4-ylpropoxy) quinazoline hydrochloride and the 3-chlorine-4- fluoroaniline are in direct reaction, the production process is simplified, the production period is shortened, energy consumption is lowered, the types of all solvents are decreased at the same time, the use level of solution medium is reduced greatly, the production cost is obviously lowered, and pollutions caused by the solvents to human body and the environment are reduced; and in the invention, by preparing formylamine solvate, the purity of prepared gefitinib is high.

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Description

technical field

[0001] The invention relates to a preparation process of high-purity gefitinib, which belongs to the technical field of pharmaceutical compound preparation. Background technique

[0002] The original preparation process of gefitinib is obtained by reacting 7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4(3H)-one in excess acyl chloride reagent 4-Chloro-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazoline hydrochloride, then evaporate under reduced pressure to remove unreacted acid chloride reagent to obtain viscous liquid 4 -Chloro-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazoline hydrochloride, the viscous liquid is neutralized with lye to obtain 4-chloro-7-methoxy -6-(3-morpholin-4-ylpropoxyl) quinazoline, then extract with organic solvent and evaporate the organic solvent under reduced pressure to obtain 4-chloro-7-methoxyl group-6-(3- Morpholin-4-ylpropoxy)quinazoline solid. Then 4-chloro-7-methoxy-6-(3-morpholin-4-ylpropoxy) quinazoline reacts with 3-chlo...

Claims

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