Table 4 Optimization of click reactiona.
Entry | Solvent | Catalyst amount (mg) | Temperature (°C) | Yield (%)b |
|---|---|---|---|---|
1 | DMF | 15 | Reflux | 45 |
2 | MeOH | 15 | Reflux | 50 |
3 | EtOAc | 15 | Reflux | 35 |
4 | THF | 15 | Reflux | 60 |
5 | Ethanol | 15 | Reflux | 70 |
6 | Water | 15 | Reflux | 20 |
7 | Ethanol/water | 15 | Reflux | 96 |
8 | Ethanol/water | 15 | 25 | 42 |
9 | Ethanol/water | 15 | 40 | 85 |
10 | Ethanol/water | 15 | 50 | 98 |
11 | Ethanol/water | 15 | 60 | 98 |
12 | Ethanol/water | 10 | 50 | 80 |
13 | Ethanol/water | 20 | 50 | 98 |