Screening of enantioselective reaction conditionsa.
| |||||
|---|---|---|---|---|---|
| Entry | Catalyst | Time (h) | Yieldb (%) | drc | eed (%) |
| 1 | C1 | 120 | 46 | >20 : 1 | 27.3 |
| 2 | C2 | 120 | 52.4 | >20 : 1 | 9.5 |
| 3 | C3 | 120 | 60 | >20 : 1 | 8 |
| 4 | C9 | 120 | 31 | >20 : 1 | 4.5 |
| 5 | C16 | 120 | 73 | >20 : 1 | 11 |
| 6 | C18 | 120 | 36 | >20 : 1 | 11 |
Reactions were carried out with 1a (0.1 mmol), 2j (0.12 mmol), and 20 mol% catalyst in 2 mL of CH3CN at rt.
Isolated yields.
Determined by 1H NMR.
Determined by HPLC analysis.