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 difficult control of cyano hydrolysis, many reaction by-products, unavoidable by-products, etc. , to avoid excessive hydrolysis, mild reaction conditions, and shorten the synthesis route
CN101463012BActive Publication Date: 2011-06-08FUJIAN SOUTH PHARMA CO LTD
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Patent Information

Authority / Receiving Office
CN Β· China
Patent Type
Patents(China)
Current Assignee / Owner
FUJIAN SOUTH PHARMA CO LTD
Publication Date
2011-06-08

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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 field of synthesis of pharmaceutical compounds, in particular to a 4-(3-chloro-4-fluorophenylamino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline ( Gefitinib) preparation method. Background technique:

[0002] 4-(3-chloro-4-fluorophenylamino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline (Gefitinib, trade name: Iressa, Iressa) is a selective inhibitor of epidermal growth factor (EGFR) tyrosine kinase, currently clinically mainly 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 (WO9633980, CN96193526) of Astrazenica Co., Ltd. The synthetic route is as follows:

[0006]

[0007] This route uses 6,7-dimethoxy-3,4-dihydroquinazolin-4-one as the raw material, uses methanesulfonic acid and L-methionine to selectively remove the 6-position methyl group, acetylation protection, and then Chlorinated, amina...

Claims

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