Screening of catalysts and reaction conditionsa,b,c.
| ||||||
|---|---|---|---|---|---|---|
| Entry | R | Catalyst | Solvent | T [°C] | %Yield | ee% |
| 1 | Me | Cat. 1 | DCM | −78 | 88 | 39 |
| 2 | Me | Cat. 2 | DCM | −78 | 87 | 42 |
| 3 | Me | Cat. 3 | DCM | −78 | 89 | 45 |
| 4 | Me | Cat. 4 | DCM | −78 | 94 | 66 |
| 5 | Me | Cat. 5 | DCM | −78 | 94 | 45 |
| 6 | Me | Cat. 6 | DCM | −78 | 90 | 67 |
| 7 | Me | Cat. 7 | DCM | −78 | 90 | 78 |
| 8 | Me | Cat. 8 | DCM | −78 | 90 | 21 |
| 9 | Me | Cat. 9 | DCM | 0 | 0 | |
| 10 | Me | Cat. 10 | DCM | 0 | 0 | |
| 11 | t Bu | Cat. 7 | DCM | −78 | 46 | 90 |
| 12 | t Bu | Cat. 7 | DCM | −20 | 56 | 95 |
| 13 | t Bu | Cat. 7 | DCM | −50 | 64 | 97 |
| 14 | t Bu | Cat. 7 | Hexane | −50 | 46 | 93 |
| 15 | t Bu | Cat. 7 | TBME | −50 | 53 | 93 |
| 16 | t Bu | Cat. 7 | Toluene | −50 | 80 | 99 |
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Reactions were conducted with 1a or 1b (0.1 mmol) and the catalyst (2 mol%) in 2 ml solvent under Ar.
Isolated yields.
Determined by HPLC analysis.