Table 3 Optimization of amination of aryl halides.
| ||||||
|---|---|---|---|---|---|---|
Entry | Cat. (mg) | Solvent | Base | Temperature (ËšC) | Time (h) | Yield (%) |
1 | - | Solvent-free | – | r.t | 1 days | N. R |
2 | 10 | Solvent-free | – | r.t | 1.5 | 71 |
3 | 20 | Solvent-free | – | r.t | 1.5 | 86 |
4 | 30 | Solvent-free | – | r.t | 1.5 | 98 |
5 | 35 | Solvent-free | – | r.t | 1.5 | 98 |
6 | 30 | EtOH | – | r.t | 1.5 | 40 |
7 | 30 | DMSO | – | r.t | 1.5 | N. R |
8 | 30 | H2O | – | r.t | 1.5 | N. R |
9 | 30 | DMF | – | r.t | 1.5 | 83 |
10 | 30 | MeOH | – | r.t | 1.5 | 85 |
11 | 30 | Solvent-free | KOH | r.t | 1.5 | 89 |
12 | 30 | Solvent-free | Na2CO3 | r.t | 1.5 | 64 |
13 | 30 | Solvent-free | Et3N | r.t | 1.5 | 88 |
14 | 30 | Solvent-free | K2CO3 | r.t | 1.5 | 85 |
