Advanced Synthesis & Catalysis · 2019 · 21 citations · 30 references
Natural SciencesChemistryOncologyCancer PharmacologyOrganic ChemistrySynthetic Medicinal ChemistryHeterocycle SynthesisHeterocyclic ChemistryBiaryl FunctionalizationFunctional Group AnalysisFunctional Group ToleranceHeterocycle FunctionalizationMedicinal HeterocyclesSelective SynthesisSelectivityTandem Reactions
Abstract An efficient palladium‐catalyzed tandem addition/cyclization of 2′‐formyl‐[1,1′‐biaryl]‐2‐carbonitriles with arylboronic acids is reported. This reaction affords dibenzo[ c , e ]azepin‐5‐ols and benzo[ c ]pyrido[2,3‐ e ]azepin‐5‐ols with excellent selectivity and wide functional group compatibility. The dibenzo[ c , e ]azepin‐5‐ols show good cell growth inhibitory activity against a triple‐negative breast cancer cell line. Moreover, the proposed mechanistic rationale for this tandem process is supported by theoretical calculations. magnified image
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Brian K. Albrecht, Victor Gehling, Michael C. Hewitt et al. · Journal of Medicinal Chemistry · 2016 · 215 citations · Full text
Medicine, Oncology, Pharmacology +15