Table 5.
Entry | α-Ketoester | 1,2-Diamine | Products | Yield (%)c | Isomers (%) |
1 | 5 | 8a | 9a | 83 | – |
2 | 5 | 8b | 9b:9b’ | 68 | 27:73 |
3 | 5 | 8c | 9c | 72 | – |
4 | 5 | 8d | 9d | 87 | – |
5a | 5 | 8e | 9e:9e’ | 65 | 44:56 |
6a | 5 | 8f | 9f:9f’ | 66 | 55:45 |
7 | 6 | 8c | 10c | 77 | – |
8 | 6 | 8d | 10d | 93 | – |
9 | 6 | 8e | 10e:10e’ | 70 | 42:58 |
10 | 6 | 8f | 10f:10f’ | 66 | 48:52 |
11 | 7 | 8a | 11a | 78 | – |
12 | 7 | 8b | 11b:11b’ | 89 | 50:50 |
13 | 7 | 8c | 11c | 91 | – |
14b | 7 | 8d | 11d | 52 | – |
15b | 7 | 8e | 11e:11e’ | 56 | 48:52 |
aReaction time of 16 h; bReaction time of 24 h. cIsolated product.