Table 3.
| ||||
---|---|---|---|---|
entry | product | R1 | R2 | yield (%)b |
1 | 4a | H | H | 87 |
2c | 4a | H | H | 80 |
3 | 4b | Me | H | 89 |
4 | 4c | H | Me | 95 |
5 | 4d | F | H | 88 |
6 | 4e | Cl | H | 80 |
7 | 4f | COOMe | H | 65 |
8 | 4g | CF3 | H | 58 |
9 | 4h | NO2 | H | 30 |
10 | 4i | CN | H | 32 |
Amine substrate (0.5 mmol) treated with PdCl2(PhCN)2 (5 mol %), Cu(NO3)2•3H2O (5 mol %) in AcOH/Ac2O (6:1, 10.5 mL) under an O2 atmosphere (1 atm) at 23 °C for 16 h.
Yield of isolated product.
Under 1 atm air instead of oxygen.