Preparation of erlotinid hydrochloride

A technology of erlotinib hydrochloride and mixed acid, applied in the field of hydrochloric acid 4--6, can solve the problems such as reducing yield and increasing steps, and achieves the effects of avoiding excessive hydrolysis, mild reaction conditions and shortening synthesis route
CN101463013BActive Publication Date: 2011-06-22FUJIAN SOUTH PHARMA CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
FUJIAN SOUTH PHARMA CO LTD
Publication Date
2011-06-22

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Abstract

The invention discloses a preparation method of erlotinib hydrochloride. The method is characterized by taking 3,4-dihydroxybenzaldehyde as a raw material, synthesizing to obtain 6,7-dimethoxyquinazoline-4-one, directly chloridizing to obtain a product, allowing the product to react with meta-ethynylaniline to obtain the erlotinib hydrochloride. The method has mild reaction condition and is applicable to industrialized production.
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Description

Technical field:

[0001] The invention relates to the field of synthesis of pharmaceutical compounds, in particular to a preparation method of 4-(3-ethynylphenylamino)-6,7-dimethoxyquinazoline hydrochloride (erlotinib hydrochloride). Background technique:

[0002] 4-(3-ethynylphenylamino)-6,7-dimethoxyquinazoline hydrochloride (erlotinib hydrochloride, Erlotinib Hydrochloride, trade name: Tarceva, Tarceva) is an epidermal growth factor (EGFR) Selective inhibitors of tyrosine kinases are currently clinically used for the treatment of non-small cell lung cancer.

[0003]

[0004] Erlotinib hydrochloride molecular structure

[0005] The synthetic route of erlotinib hydrochloride is mainly Schnur of U.S. Pfizer Inc.N.Y., Rodney.C. etc. report (US5747498), and its synthetic route is as follows:

[0006]

[0007] This route uses ethyl 3,4-dihydroxybenzoate as a raw material, first reacts with bromoethyl methyl ether, then nitrates, reduces nitro to amino, cyclizes, chlorate...

Claims

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