Screening for solvents for chiral catalyst.
| |||||
|---|---|---|---|---|---|
| Entry | Solvent | Temp (°C) | Time (h) | Yield (%) of 15aa,b | eec (%) |
| 1 | DCM | Rt | 8 | 87 | 94.0 |
| 2 | Toluene | Rt | 10 | 90 | 94.2 |
| 3 | H2O | Rt | 24 | 88 | 65.2 |
| 4 | U/CC 2 : 1 | Rt | 20 | 87 | 94.8d |
| 5 | U/CC 2 : 1 | 60 | 12 | 90 | 22.3 |
Yields refer to pure and isolated 15a.
The reaction was carried out with 1 mmol of 12a, 13a, 14a and 5 mol% of catalyst 11.
Ee was determined by chiral analyses on HPLC.
The same results were obtained using 10 mol% of catalyst 11.