Scope of substratesa.
| |||||||
|---|---|---|---|---|---|---|---|
| Entry | 1 | R1 | R2 | R3 | 3 | [M]X | Yield of 3 b (%) |
| 1c | 1b | MeO | H | H | 3b | Cu(NTf2)2 | 44 |
| 2 | 1c | Me | H | H | 3c | Cu(NTf2)2 | 47 |
| 3 | 1d | Br | H | H | 3d | Cu(NTf2)2 | 77 |
| 4 | 1e | CF3 | H | H | 3e | AgNTf2 | 72 |
| 5 | 1f | H | MeO | H | 3f | AgNTf2 | 39 |
| 6 | 1g | H | Me | H | 3g | Cu(NTf2)2 | 58 |
| 7 | 1h | H | Br | H | 3h | AgNTf2 | 59 |
| 8 | 1i | H | CF3 | H | 3i | Cu(NTf2)2 | 63 |
| 9 | 1j | H | H | Me | 3j | AgNTf2 | 74 |
Unless otherwise specified, all reactions were carried out using 0.1 mmol of 1, 1.0 mmol (10 equiv.) of 2a, 10 μmol (10 mol%) of AgNTf2 or Cu(NTf2)2, 20 μmol (20 mol%) of P(4-CF3C6H4)3, and 5 equiv. of TFA in 1,2-dichloroethane (1 mL: 0.1 M of 1) at 50 °C for 1 h.
Isolated yield.
At 0 °C for 6 h.