1130155-48-4Relevant articles and documents
A EGFR molecule targeting anti-tumor pharmaceutical preparation method
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Paragraph 0027-0029, (2019/05/06)
The invention relates to a preparation method for an EGFR molecule targeting antitumor drug, and provides a preparation method for (E)-N-[4-(3-acetylene phenyl)amino-3-cyan-7-ethoxy-6-quinolyl]-4-(dimethyl amino)-2-butylene amide. The preparation method comprises the following steps: N-(4-chloro-3-cyan-7-ethoxy quinoline-6-yl) acetamide (a compound II) and 3-aminophenylacetylene (a compound III) are subjected to a substitution reaction, and a compound IV is obtained; under an acidic or alkaline condition, the compound IV is subjected to a hydrolysis reaction, and 3-cyan-6-amino-7-ethoxy-4-(3-acetenyl anilino) quinoline (a compound V) is obtained; after trans-4-dimethylaminocrotonic acid hydrochloride (a compound VI) and an acylation reaction reagent is subjected to an acylation reaction, the product and 3-cyan-6-amino-7-ethoxy-4-(3-acetenyl anilino) quinoline (the compound V) are subjected to condensation reaction, and the finished product is obtained. The method is advantageous in that raw materials are easily available, the technology is concise, the production cost is low, and the method is economical and environmentally friendly and is suitable for industrial production.
Synthetic method for (2Z)-4-(dimethylamino)but-2-enoic acid hydrochloride
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Paragraph 0026-0035, (2018/11/02)
The invention discloses a synthetic method for (2Z)-4-(dimethylamino)but-2-enoic acid hydrochloride. The synthetic method comprises the following steps: under an inert gas atmosphere, dissolving [bi(2,2,2-trifluoroethoxy)-phosphinyl]methyl acetate in organic solvent, adding lithium reagent, adding alkali solution, controlling the temperature to 0-30 DEG C, adding 2-(dimethylamino)acetaldehyde sulfite, and carrying out stirring reaction, carrying out acidification, extraction and column purification after reaction to obtain the (2Z)-4-(dimethylamino)but-2-enoic acid hydrochloride. The syntheticmethod has the advantages of convenience in operation and high yield, and industrial production can be realized.
QUINAZOLINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF
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Paragraph 0134; 0137, (2017/07/14)
Disclosed are a quinazoline derivative, a preparation method therefor, and a pharmaceutical composition and an application thereof. The present invention provides a compound represented by general formula I, a stereoisomer thereof and a pharmaceutical acceptable salt or a solvate thereof. The quinazoline derivative of the present invention has a unique chemical structure, is characterized by irreversibly inhibiting EGFR tyrosine kinase, has high biological activity, apparently improves the inhibiting effect on the EGFR tyrosine kinase, has quite strong tumor inhibiting effect on tumor cells and a transplantation tumor pathological model of animal tumors, and has good market developing prospects.