Table 1.
Entry | Solvent | Temp (°C) | Yield b (%) |
---|---|---|---|
1 | 1,4-dioxane | 80 | 33 |
2 | THF | 80 | 42 |
3 | CH3CN | 80 | 31 |
4 | Toluene | 80 | 17 |
5 | Methanol | reflux | 57 |
6 | Ethanol | 80 | 68 |
7 | Ethanol/H2O | 100 | 55 |
8 | Ethanol | 50 | 74 |
9 c | Ethanol | 50 | 95 |
a Unless indicated otherwise, the reaction was performed with 3a (0.5 mmol), 1a isatin (0.5 mmol), and L-proline (0.5 mmol) in different solvents (10.0 mL) and temperatures for 5 h. b Isolated yield based on isatin. c 10 h.