Table 1.
no. | R1 | R2 | R3 | yield,a % | ||
---|---|---|---|---|---|---|
1 | Cl | Ph | 1a | Ph | 3a | 81 |
2 | Cl | Ph | 1a | p-OMeC6H4 | 3b | 79 |
3 | Cl | Ph | 1a | p-CO2MeC6H4 | 3c | 65 |
4 | Br | Ph | 1b | Ph | 3d | 88b |
5 | Cl | p-OMeC6H4 | 1c | Ph | 3e | 67 |
6 | Cl | p-OMeC6H4 | 1c | o-tolyl | 3f | 45 |
7 | Cl | p-CF3C6H4 | 1d | Ph | 3g | 68 |
8 | Cl | p-CF3C6H4 | 1d | 1-cyclohexenyl | 3h | 93 |
9 | Cl | CO2Me | 1e | p-tolyl | 3i | 93c |
10 | Cl | CO2Me | 1e | p-OMeC6H4 | 3j | 67 |
11 | Cl | CO2Me | 1e | p-CO2MeC6H4 | 3k | 72 |
12 | Cl | CO2Me | 1e | m-CO2MeC6H4 | 3l | 87 |
13 | Br | Ph | 1b | n-butyl | 3m | 69 |
14 | Cl | CO2Me | 1e | Ph | 3n | 86d |
15 | Cl | Ph | 1a | (CH2)3Cl | 3o | 68 |
Isolated yield.
8% ee.
86% ee.
84% ee.