Table 1. Optimization of the Reaction Conditionsa.
| entry | 1a/2a | solvent | yield (%) |
|---|---|---|---|
| 1 | 1.0/1.0 | H2O | 19 |
| 2 | 1.0/1.5 | H2O | 67 |
| 3 | 1.0/2.0 | H2O | 70 |
| 4 | 1.0/3.0 | H2O | 73 |
| 5 | 1.0/2.0 | nBuOAc | 12 |
| 6 | 1.0/2.0 | DMF | 22 |
| 7 | 1.0/2.0 | toluene | N.R. |
| 8 | 1.0/2.0 | PhCl | trace |
| 9b | 1.0/2.0 | H2O | 32 |
Reaction conditions: 1a (0.3 mmol), solvent (3 mL), 120 °C (oil bath), 24 h, under air.
9 h.
