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

A synthesis method and substituent technology, applied in the field of synthesis of quinazoline derivatives, 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: 2012-10-24
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
  • Synthesis method of 6, 7-substituted-4-aniline quinazoline
  • 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-substituent-4-aniline quinazoline; another synthetic route must go through hydrolysis-demethylation reaction, and its synthetic steps include esterification reaction, oxygen-alkylation reaction or nitration reaction, hydrolysis -Demethylation reaction, esterification reaction, oxygen-alkylation reaction, nitro...

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Abstract

The invention relates to a synthesis method of 6, 7-substituted-4-aniline quinazoline. The reaction path of the synthesis method comprises the following steps of: performing esterification, oxygen-alkylation reaction or nitration reaction on 3-methoxyl-4-hydroxybenzoic acid serving as an initiator,, performing hydrolysis-demethylation reaction, esterification, oxygen-alkylation reaction, nitroreduction reaction, cycling reaction, two-in-one reaction and other steps after nitration so as to prepare the 6, 7-substituted-4-aniline quinazoline. The invention provides the preparation way of a 4-aniline quinazoline derivative, which has the advantages of lower cost of the initiator and higher yield, so that the production cost can be effectively reduced and the competitiveness of products of 4-aniline quinazoline derivatives can be improved.

Description

technical field [0001] The present invention relates to a synthesis method of quinazoline derivatives, in particular to a synthesis method of 6,7-substituent-4-aniline quinazoline. The present invention is a divisional application of Chinese patent application CN200910133962.3. 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 (Gefitinib), Erlotinib (Erlotinib) and the drug Vandetta for the treatment of lung cancer and thyroid cancer (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 abou...

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Application Information

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