A kind of preparation method of EGFR molecular targeted anti-tumor drug

A cyano- and ethoxy-based technology, which is applied in antineoplastic drugs, drug combinations, organic chemistry, etc., can solve the problems of high impurity content, difficult quality control, and low conversion rate of Compound IV, and achieve easy-to-obtain raw materials and reduce The content of impurities and the effect of low production cost
CN111875539BActive Publication Date: 2022-06-21JIANGSU SUZHONG PHARM GRP CO LTD +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
JIANGSU SUZHONG PHARM GRP CO LTD
Publication Date
2022-06-21

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Abstract

The invention discloses a preparation method of an EGFR molecule-targeted antitumor drug, and the EGFR molecule-targeted antitumor drug is (E)-N-[4-(3-ethynylphenyl)amino-3- Cyano-7-ethoxy-6-quinolyl]-4-(dimethylamino)-2-butenamide. The preparation method of the EGFR molecular targeting antineoplastic drug comprises the following steps: N-(4-chloro-3-cyano-7-ethoxyquinoline-6-yl) acetamide and m-aminophenylacetylene Under the condition of n-propanol as reaction solvent, heating substitution reaction was carried out. The method has the advantages of easy-to-obtain raw materials, simple process, short reaction time, low impurity content, high yield, and suitability for industrialized production.
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Description

technical field

[0001] The invention belongs to the technical field of organic synthesis route design and preparation of bulk drugs and intermediates, in particular to a (E)-N-[4-(3-ethynylphenyl)amino-3-cyano-7-ethoxy group -The preparation method of 6-quinolinyl]-4-(dimethylamino)-2-butenamide. Background technique

[0002] (E)-N-[4-(3-Ethynylphenyl)amino-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide , and its structural formula is:

[0003]

[0004] (E)-N-[4-(3-Ethynylphenyl)amino-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide (I) is a new type of EGFR-targeted anti-tumor drug jointly developed by Jiangsu Suzhong Pharmaceutical Group Co., Ltd. and Jiangsu Maidu Drug Research and Development Co., Ltd., which is an irreversible pan-ErbB receptor tyrosine kinase inhibitor , can effectively inhibit ErbB1 and ErbB2 tyrosine kinase activity, mainly used for the treatment of non-small cell lung cancer (Non Small Cell Lung Cancer, NSCLC). [...

Claims

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