Table 2.
Reductive amination of benzaldehydesa
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|---|---|---|---|---|---|
| Entry | Aldehyde | 2 (%)b | 3 (%)b | 4 (%)b | |
| 1 | 1a | R = H | 81 (72c) | <1 | 18 |
| 2 | 1b | R = p-OMe | 79 (92c) | <1 | 21 |
| 3 | 1c | R = p-Br | 87 (73c) | 2 | 11 |
| 4 | 1d | R = m-Br | 72 (84c) | 7 | 21 |
| 5 | 1e | R = o-Br | 97 (89c) | 3 | <1 |
| 6 | 1f | R = p-Cl | 98 (90c) | <1 | <1 |
| 7 | 1g | R = p-F | 48 | 26 | 26 |
| 8 | 1h | R = p-NO2 | 87(81c) | 4 | 9 |
| 9 | 1i | R = m-NO2 | 86 | 4 | 10 |
| 10 | 1j | R = o-NO2 | 71 | 8 | 21 |
| 11 | 1k | R = p-CN | 63 | 9 | 28 |
Reagents and conditions: aldehyde (100 μmol), Ir1 (1.0 μmol), HCOONH4 (1.0 mmol), CH3OH (0.5 mL), 37 °C, 15 h.
Determined by 1H NMR with 1,3,5-trimethoxybenzene as internal standard, each experiment was performed in triplicate and the average yield was calculated.
Isolated yield. Some isolated yields of 2 were higher than their NMR yields because compound 4 was hydrolyzed to 2 during the workup step.
