Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume 74, Issue 16, Pages 6354-6357Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jo9010624
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Introduction of oxetan-3-yl and azetidin-3-yl groups into heteroaromatic bases was achieved by using a radical addition method (Minisci reaction). To demonstrate utility. the process was used to introduce an oxetane Or azetidine into heteroaromatic systems that have found important uses in the drug discovery industry, such as the marketed EGFR inhibitor geftinib, a quinolinecarbonitrile Src tyrosine kinase inhibitor, and the antimalarial hydroquinine.
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