Preparation of gefitinib

A technology of gefitinib and compounds, applied in the field of preparation of 4--7-methoxy-6-quinazoline, which can solve the problems of many reaction by-products, difficult control of cyano hydrolysis, unavoidable by-products, etc. , to avoid excessive hydrolysis, shorten the synthesis route, and achieve the effect of mild reaction conditions
CN101463012AActive Publication Date: 2009-06-24FUJIAN SOUTH PHARMA CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
FUJIAN SOUTH PHARMA CO LTD
Publication Date
2009-06-24

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Abstract

The invention discloses a preparation method of gefitinib. In the method, isovanillin is taken as a raw material and synthesized to obtain 7-methoxy-6-(3-morpholine-propoxy)quinazoline-4-one which is directly chloridized to obtain a product, the product is allowed to react with 3-chlorine-4-fluoroaniline to obtain gefitinib hydrochloride which neutralized off hydrochloric acid to obtain the gefitinib. The method has mild reaction condition and is applicable to industrialized production.
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Description

Technical field:

[0001] The present invention relates to the synthetic field of pharmaceutical compounds, in particular to a kind of 4-(3-chloro-4-fluorophenylamino)-7-methoxy-6-(3-morpholine propoxy)quinazoline ( Gefitinib) preparation method. Background technique:

[0002] 4-(3-Chloro-4-fluorophenylamino)-7-methoxy-6-(3-morpholine propoxy)quinazoline (Gefitinib, Gefitinib, trade name: Iressa, Iressa) is a selective inhibitor of epidermal growth factor (EGFR) tyrosine kinase, and is currently clinically used for the treatment of non-small cell lung cancer.

[0003]

[0004] Gefitinib molecular structure

[0005] The synthetic route of gefitinib is mainly reported by K.H. Gibson of Astra Zenica Co., Ltd. (WO9633980, CN96193526), ​​and its synthetic route is as follows:

[0006]

[0007] This route uses 6,7-dimethoxy-3,4-dihydroquinazolin-4-one as raw material, selectively removes the 6-position methyl group with methanesulfonic acid and L-methionine, protects by ace...

Claims

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