Table 1.
Entry | THIQ (equiv) | Solvent | T (°C) | Time (min) | Yield (%) | dr |
---|---|---|---|---|---|---|
1 | 1.3 | PhMe | reflux | 60 | 56 | 1:1 |
2 | 1.3 | DCE | reflux | 60 | 58 | 1.3:1 |
3b | 1.3 | PhMe | 150 | 5 | 61 | 1.1:1 |
4b | 1.3 | DCE | 150 | 5 | 76 | 1:1 |
5b | 2.0 | DCE | 150 | 5 | 61 | 1.1:1 |
6b | 1.3 | DCE | 100 | 5 | 71 | 1.4:1 |
7b | 1.3 | DCE | 100 | 15 | 75 | 1.2:1 |
Reactions were performed on a 0.25 mmol scale. All yields correspond to isolated yields. The dr was determined by 1H NMR analysis after purification.
Performed under microwave irradiation.