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Synthesis method of 6,7-substituted-4-aniline quinazoline

A synthetic method and substituent technology, applied in 6 fields, can solve the problems of expensive raw materials, complicated reaction steps, unstable intermediate products, etc., and achieve the effect of reducing production costs and improving competitiveness

Inactive Publication Date: 2010-10-20
OMEGA MEDICAL TAIWAN
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Problems solved by technology

[0015] However, in the above-mentioned method for preparing 6,7-substituent-4-aniline quinazolines, there are problems such as expensive raw materials, complicated reaction steps, unstable intermediate products or low yields.

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  • Synthesis method of 6,7-substituted-4-aniline quinazoline

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[0034] In order to make the above and other objects, features and advantages of the present invention more comprehensible, the following will be described in detail with the accompanying drawings.

[0035] The invention discloses a method for synthesizing 6,7-substituent-4-aniline quinazolines using 3,4-substituted benzoic acid (3,4-substituted benzoic acid) as a starting material; wherein, a synthesis method It can be prepared through esterification reaction, oxygen-alkylation reaction, nitration reaction, nitro reduction reaction, cyclization reaction and two-in-one reaction (one-pot reaction) without going through the hydrolysis-demethylation reaction step. Obtain 6,7-substituting group-4-aniline quinazoline; Another synthetic route must go through hydrolysis-demethylation reaction, and its synthesis step comprises esterification reaction, oxygen-alkylation reaction or nitration reaction, hydrolysis -Demethylation reaction, esterification reaction, oxygen-alkylation reactio...

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Abstract

The invention relates to a synthesis method of 6,7-substituted-4-aniline quinazoline. In the method, substances such as 3,4-substituted benzoic acid, and the like are used as starting materials, and the 6,7-substituted-4-aniline quinazoline is prepared through a reaction path of esterification reaction, oxygen-alkylation reaction, nitration reaction, nitro reduction reaction, ring closing reaction and two-in-one reaction or a reaction path of esterification reaction, oxygen-alkylation reaction or nitration reaction, hydrolysis-demethylation reaction after the nitration reaction, esterification reaction, oxygen-alkylation reaction, nitro reduction reaction, ring closing reaction, two-in-one reaction, and the like. The invention also provides a preparation method of a 4-aniline quinazoline derivative with lower starting material cost and higher productivity, which can effectively reduce the production cost so as to improve the competitiveness of a 4-aniline quinazoline derivative product.

Description

technical field [0001] The present invention relates to a synthesis method of quinazoline derivatives, and in particular to a synthesis method of 6,7-substituent-4-aniline quinazolines. Background technique [0002] Epidermal Growth Factor Receptor (EGFR, Epidermal Growth Factor Receptor) plays an important role in the development of cancer, and 6,7-substituent-4-aniline quinazolines are also widely used clinically mainly for non-small cell The treatment of lung cancer (Non-small-cell lung cancer, NSCLC), such as the marketed drugs Gefitinib, Erlotinib, and the drug Vandetta for the treatment of lung and thyroid cancer Vandetanib is also used for the treatment of Myeloid leukemia or Myelodysplasia in the second clinical phase, such as Tandutinib, whose structure is as follows: [0003] [0004] There are many literature reports about the improved synthesis of 6,7-substituent-4-aniline quinazolines, such as: [0005] 1. WO 2004024703 [0006] Starting with Isovanilln, u...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/94C07D401/12A61P35/00A61P35/02
CPCC07D401/12C07D239/94A61P35/00A61P35/02
Inventor 施凯翔谢幼容刘清维
Owner OMEGA MEDICAL TAIWAN
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