- Preparation method of EGFR molecular targeting antitumor drug
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The invention discloses a preparation method of an EGFR molecular targeting antitumor drug. The EGFR molecular targeting antitumor drug is (E)-N-[4-(3-acetylenephenyl)-amino-3-cyano-7-ethoxy-6-quinolyl]-4-(dimethylamino)-2-buteneamide. The preparation method of the EGFR molecular targeting antitumor drug comprises the following step: carrying out a heating substitution reaction on N-(4-chloro-3-cyano-7-ethoxyquinoline-6-yl)acetamide and m-aminophenylacetylene under the condition that n-propanol is used as a reaction solvent. The method has the advantages of easily available raw materials, simple process, short reaction time, low impurity content, high yield, suitability for industrial production and the like.
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Paragraph 0073-0078; 0091-0096
(2020/11/22)
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- A EGFR molecule targeting anti-tumor pharmaceutical preparation method
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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.
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Page/Page column 6-8; 9; 10
(2019/05/06)
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- SUBSTITUTED HETEROCYCLIC COMPOUNDS AS KINASES INHIBITORS AND METHOD OF USE THEREOF
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The present invention is directed to novel quinolines and quniazolines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof which are useful for the treatment of protein kinases mediated diseases and conditions. The compounds of this invention have a general Formula (I) wherein R1 to R11 and X are defined herein.
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Page/Page column 35
(2011/01/12)
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