Table 16.
Asymmetric intermolecular aza-Michael addition of (E)-3-substituted-2-enoic acid.
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71 | R | Yield [%] | ee [%] |
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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 | – |