Table 16.
Asymmetric intermolecular aza-Michael addition of (E)-3-substituted-2-enoic acid.
| |||
|
| |||
| 71 | R | Yield [%] | ee [%] |
|
| |||
| a | Me | 75 | 97 |
| b | Et | 84 | 90 |
| c | Pr | 72 | 90 |
| d | n-C5C11 | 76 | 88 |
| e | n-C7C15 | 75 | 86 |
| f | CH(CH3)2 | 57 | 76 |
| g | CH2-OBn | 89 | 85 |
| h | (CH2)3-OBz | 86 | 91 |
| i | (CH2)2-SMe | 78 | 87 |
| j | (CH2)3-NHCbz | 80 | 71 |
| k | (CH2)2-C6H4-CF3-4 | 76 | 83 |
| l | (CH2)2-C6H4-MeO-4 | 88 | 87 |
| m | (CH2)2-C6H4-Br-2 | 85 | 88 |
| n | (CH2)2-C6H3-3,4-(OMe)2 | 81 | 86 |
| o | (CH2)2-2-naphthyl | 90 | 87 |
| p | (CH2)3-Ph | 81 | 91 |
| q | (CH2)4-Ph | 84 | 88 |
| r | CH2-Ph | 80 | 71 |
| s | Ph | 0 | – |