Table 2.
Entry | Catalyst | R1 | R2 | R3 | R4 | R5 | Yield (%) 2 |
---|---|---|---|---|---|---|---|
1 | LSA-Sc3+ | Br | H | H | H | H | 93 (90) |
2 | LSA-Sc3+ | Br | H | H | H | Me | 98 |
3 | LSA-Sc3+ | Br | H | H | OMe | H | 97 |
4 | LSA-Sc3+ | Br | H | H | Br | H | 61 |
5 | LSA-Sc3+ | Br | H | Me | H | H | 93 |
6 | LSA-Sc3+ | Br | H | H | H | Ph | 85 3 |
7 | LSA-Sc3+ | Cl | H | H | H | H | 96 |
8 | LSA-Sc3+ | Cl | H | H | H | Me | 96 |
9 | LSA-Sc3+ | H | H | H | H | H | 93 |
10 | LSA-Sc3+ | OMe | H | H | H | H | 86 |
11 | LSA-Sc3+ | tBu | H | H | H | H | 96 |
12 | LSA-Sc3+ | H | Me | H | H | H | 68 |
13 | LSA-Sc3+ | H | OMe | H | H | H | 61 |
14 | LSA-Sc3+ | Me | Me | H | H | H | 83 |
15 | SiO2-Sc3+ | Br | H | H | H | H | 92 (50) |
16 | resin-Sc3+ | Br | H | H | H | H | 87 (63) |
1 Reaction conditions: 3-acetyl-2-hydroxy-2-methylchromene derivative (0.5 mmol), indole derivative (0.6 mmol), LSA-Sc3+ (1.2 mol%), EtOH (1 mL), 80 °C, 8 h. Isolated yields. The yield in parentheses shows the reuse of the catalyst in the third run. 2 Isolated yield. 3 Catalyst amount = 2 mol%. 1-Methyl-2-phenyl-1H-indole was used as the Michael donor.