Table 1. Reaction Optimizationa.
Standard reaction conditions: 1 (0.20 mmol), p-TolI (20 mol %), Selectfluor (0.30 mmol), Py·HF (4–16 mmol), Et3N (0.22–1.50 mmol), DCE (0.50 mL), 24 h, room temperature.
Yield and dr determined by 19F NMR with α,α,α-trifluorotoluene as an internal standard.
p-TolI was excluded from the reaction mixture.
0.50 mmol scale.
Isolated yield.
Heated to 50 °C.