Adam J. Close, Rhiannon N. Jones, Cory A. Ocasio
Sep 1, 2016
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Influential Citations
2
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Journal
Organic & biomolecular chemistry
Abstract
Nitration of three regioisomers of bromo-fluorobenzaldehyde proceeds regioselectively, notably with H2SO4/HNO3 at 0 °C. The thereby synthesized tetrasubstituted aromatics, endowed with orthogonal substituents, can be elaborated via Pd-catalysed coupling, reduction and reductive amination reactions. As a test-case, these compounds were converted into EGFR inhibitors related to Gefitinib, whose activity was rationalised by docking studies.