Table 2.
Generality of amine precursors in aminoheteroarylation reactions
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Reaction conditions: 1 (0.2 mmol, 1.0 equiv), 4 (2.0 equiv), Cu(OTf)2 (10 mol %), TsOH∙H2O (1.5 equiv), DCE (1 mL), 80 °C. Isolated yields shown.
Run with 4f (3.0 equiv).
Run at 40 °C.
Run with 4j (4.0 equiv) and TsOH∙H2O (3.0 equiv) at 60 °C.
Run at 40 °C.
Run with 4n (3.0 equiv) and TsOH∙H2O (2.25 equiv) at 60 °C.
Run with 1b (0.1 mmol, 1.0 equiv), 4o (3.0 equiv) and TsOH∙H2O (6.0 equiv).