Elaboration of tetra-orthogonally-substituted aromatic scaffolds towards novel EGFR-kinase inhibitorsElectronic supplementary information (ESI) available. CCDC 1485121-1485123. For ESI and crystallographic data in CIF or other electronic format see DOI: 10.1039/c6ob01394e

Nitration of three regioisomers of bromo-fluorobenzaldehyde proceeds regioselectively, notably with H 2 SO 4 /HNO 3 at 0 °C. The thereby synthesized tetrasubstituted aromatics, endowed with orthogonal substituents, can be elaborated via Pd-catalysed coupling, reduction and reductive amination reacti...

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Hauptverfasser: Close, Adam J, Jones, Rhiannon N, Ocasio, Cory A, Kemmitt, Paul, Roe, S. Mark, Spencer, John
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