Table 1.
Optimization of reaction conditions.[a]
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|---|---|---|---|---|
| Entry | Imine (R1) | Solvent | Yield [%][b] | ee [%][c] |
| 1 | 2a (Ph) | toluene | 4a: 88 | 75 |
| 2 | 2a | CH2Cl2 | 4a: 88 | 79 |
| 3 | 2a | THF | 4a: 86 | 47 |
| 4 | 2a | EtOAc | 4a: 93 | 84 |
| 5 | 2a | iPrOAc | 4a: 84 | 86 |
| 6 | 2b (4-MeOC6H4) | iPrOAc | 4b: 83 | 90 |
| 7 | 2c (2-MeC6H4) | iPrOAc | 4c: 92 | 84 |
| 8 | 2d (3-MeC6H4) | iPrOAc | 4d: 83 | 88 |
| 9 | 2e (3-MeOC6H4) | iPrOAc | 4e: 82 | 97 |
| 10 | 2 f (3,5-(MeO)2C6H3) | iPrOAc | 4 f: 81 | 96 |
Reaction conditions: imine 2a–f (0.1 mmol), hydroperoxide 3a (0.2 mmol), (R)-1 (5 mol%), solvent (0.6 mL) at room temperature.
Yield of isolated product.
Determined by HPLC analysis using a chiral stationary phase.
