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Optimization of reaction conditionsa.
 | |||
|---|---|---|---|
| Entry | Solvent/T (°C) | Time (h) | Yield (%) |
| 1 | MeCN/20 | 20 | 10 |
| 2 | MeCN/50 | 12 | 58 |
| 3 | EtOAc/50 | 24 | 45 |
| 4 | MeCN/reflux | 1.5 | 96 |
| 5 | EtOAc/reflux | 12 | 60 |
| 6 | DCM/reflux | 8 | 25 |
| 7 | THF/reflux | 5 | 39 |
| 8 | Benzene/reflux | 5 | 64 |
| 9 | Dioxane/reflux | 5 | 50 |
Reaction conditions: 1 (1 mmol) and 2a (1.1 mmol) in a solvent (5 mL) at the indicated reaction conditions. Bold value indicates the best condition of the reaction.
