Table 1.
| |||||
---|---|---|---|---|---|
entrya | azide {G} (equiv.) | amine 6 (equiv.) | CuI (mol %) | DBU (mol%) | yield (%) |
1 | 2 | 2 | 10 mol% | 10 mol% | 62 % |
2 | 2 | 2 | 30 mol% | 10 mol% | 96 % |
3 | 1 | 1 | 30 mol% | 10 mol% | 78 % |
4 | 2 | 1.2 | 30 mol % | 10 mol% | 95 % |
5 | 2 | 1.2 | 30 mol% | 10 mol% | 96 % |
Reactions carried out utilizing 2 (50 mg, 0.32 mmol, 1 equiv.) in 0.5 M EtOH at 60 °C for 12 hrs.