4-oxo-7-methoxy-1,4-dihydroquinoline-6-methyl formate synthesis method

A technology of methyl methoxybenzoate and methyl nitrobenzoate, which is applied in the field of pharmaceutical synthesis and achieves the effects of improving the utilization efficiency of raw materials, high yield, and being conducive to enlarged production
CN106543080AActive Publication Date: 2017-03-29SHANDONG BOYUAN PHARM CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANDONG BOYUAN PHARM CO LTD
Publication Date
2017-03-29

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Abstract

The invention relates to a 4-oxo-7-methoxy-1,4-dihydroquinoline-6-methyl formate synthesis method. The method includes that 4-nitro-methyl-2-methoxybenzoate which is taken as a starting material is subjected to friedel-crafts reaction, reduction and ammonolysis cyclization to obtain a target compound. By adoption of classic reaction, a step of decarboxylation in diphenyl ether at a high temperature of 180-220 DEG C in an existing universal method is avoided, problems in production are solved, safety and environment friendliness are achieved, and production enlargement is benefited. In addition, the synthesis method has advantages of high reaction efficiency, high yield, high purity, low cost and the like.
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Description

technical field

[0001] The invention relates to a method for synthesizing lenvatinib intermediate 4-oxo-7-methoxy-1,4-dihydroquinoline-6-carboxylic acid methyl ester, belonging to the technical field of drug synthesis. Background technique

[0002] Lenvatinib, the chemical name is 4-[3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxy-6-quinolinecarboxamide, and its structural formula is as follows:

[0003]

[0004] It is an orally effective multi-kinase inhibitor developed by Eisai Corporation of Japan, targeting vascular endothelial growth factor receptor (VEGFR) 1-3, fibroblast growth factor receptor (FGFR) 1-3, stem cell Growth factor receptor and beta-type platelet-derived growth factor receptor (PDGFR). It is used for the treatment of solid tumors such as glioma, thyroid tumor, renal cancer, liver cancer and ovarian cancer, and it is preferred for differentiated thyroid cancer that cannot be treated by radioactive iodine. In February 2013, it was approve...

Claims

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