Table 1.
| |||||
---|---|---|---|---|---|
entry | 5 | R1 | R2 | yielda | er/drb |
1 | a | H | Ph | 80 | 97:3 |
2 | b | Me | Ph | 65 | 96:4 |
3 | c | Ph | Ph | 72 | 96:4 |
4 | d | CF3 | Ph | 78 | 97:3 |
5 | e | H | Bn | 69 | 94:6 |
6 | f | Me | Bn | 62 | 92:8 |
7 | g | Ph | Bn | 70 | 93:7 |
8 | h | CF3 | Bn | 71 | 96:4 |
9c | i | Ph | (R)-CH(Me)Ph | 76 | 88:12 |
10c | j | Ph | (S)-CH(Me)Ph | 74 | 20:80 |
Isolated yields, an average of three experiments generally exhibiting a spread of ±2%.
Enantiomer ratio (er) determined by chiral HPLC analysis or diastereomer ratio (dr) determined by 1H NMR.
2% catalyst loading.