Table 1.
Optimization of the reaction conditionsa.
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| Entry | Solvent | Temperature | Time, h | Yield, % |
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| 1 | MeCN | reflux | 0.5 | 15 |
| 2 | MeCN | reflux | 3 | 22 |
| 4 | MeCN | reflux | 6 | 18 |
| 5 | MeCN | rt | 3 | 13 |
| 6 | MeCN | rt | 12 | 44 |
| 7 | MeCN | rt | 24 | 62 |
| 8 | MeCN | rt | 48 | 61 |
| 9 | dioxane | rt | 24 | 54 |
| 10 | toluene | rt | 24 | 49 |
| 11 | CH2Cl2 | rt | 24 | 51 |
aReaction conditions: 3a (0.37 g, 1 mmol), CDI (0.49 g, 3 mmol), DBU (0.17 g, 1.1 mmol), solvent (7 mL).