An alternative synthesis of the non-small cell lung carcinoma drug afatinib
Tetrahedron Letters(2018)
摘要
•The alternative synthesis of afatinib (BIBW2992) is presented.•The work is presenting a new route with good yield that could be suitable for industrial use.•Ullmann-Goldberg reaction for CN coupling on position 6 of quinazoline.•The synthesis provides direct access to afatinib analogues of and similar quinazoline type of kinase inhibitors.
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关键词
Afatinib,EGFR inhibitor,CN coupling,Quinazolinon,Ullmann-Goldberg
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