Journal
TETRAHEDRON LETTERS
Volume 59, Issue 47, Pages 4180-4182Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2018.10.026
Keywords
Afatinib; EGFR inhibitor; C-N coupling; Quinazolinon; Ullmann-Goldberg
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Afatinib (BIBW2992) is the anticancer drug developed by Boehringer Ingelheim. This work is reporting the synthesis of the afatinib using a new route by Ullmann-Goldberg reaction from corresponding 4-anilinoquinazoline iodide as the last step in the synthesis. This route was not described previously and it could be used for synthesis of afatinib analogues. (C) 2018 Elsevier Ltd. All rights reserved.
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