78554-68-4Relevant articles and documents
Preparation method of icotinib key intermediate
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Paragraph 0039; 0040; 0041, (2020/07/15)
The invention discloses a preparation method of an icotinib key intermediate, and belongs to the technical field of drug synthesis. According to the preparation method, triethylene glycol(p-toluene sulfonate) and N-Boc-3,4-dihydroxyl aniline are used as raw materials; the raw materials carry out crown ether cyclization reaction, halogenation reaction and amination reaction (amidation reaction), quinoline cyclization reaction, and chlorination reaction to obtain an icotinib key intermediate, namely 4-chloro-quinazoline[6.7-6]-12-crown-4; the newly designed synthesis route does not need a strongacid solution, which is required by a conventional synthesis route; the dangerous operation is avoided, the generation of a large amount of acidic waste liquid is avoided; and the novel synthesis route has the advantages of simple operation and high yield.