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Asymmetric aza-Michael–Henry cascade reaction.
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| 45 | R1 in 42 | R2 | Yield [%]a | ee [%]b |
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| a | H | 2,3-(MeO)2-C6H3 | 67 (65) | 98 (98) |
| b | H | 4-Me-C6H4 | 60 (59) | 90 (93) |
| c | H | 2,4-(Cl)2-C6H3 | 45 (40) | 97 (96) |
| d | H | 3,4-(Cl)2-C6H3 | 42 (38) | 95 (97) |
| e | 3-MeO | Ph | 52 (50) | 95 (99) |
| f | 5-Cl | Ph | 55 (53) | 98 (99) |
| g | 3,5-Br2 | Ph | 68 (67) | 99 (98) |
aDetermined by 1H NMR. bDetermined by HPLC. The data in parentheses are reproduced results.
