Table 2.
Domino synthesis of bis-indoles 5 under MWa
| Entry | 5 | Ar | Ar′ | Time/ min | Yieldb/ % |
|---|---|---|---|---|---|
| 1 | 5a | 4-Tolyl (1g) | Phenyl (2a) | 30 | 51 |
| 2 | 5b | 4-Tolyl (1g) | 4-Fluorophenyl (2c) | 28 | 54 |
| 3 | 5c | 4-Tolyl (1g) | 4-Chlorophenyl (2d) | 26 | 50 |
| 4 | 5d | 4-Tolyl (1g) | 4-Bromophenyl (2e) | 26 | 52 |
| 5 | 5e | 4-Tolyl (1g) | 4-Methoxyphenyl (2f) | 30 | 48 |
| 6 | 5f | 4-Tolyl (1g) | 3-Methoxyphenyl (2g) | 30 | 45 |
| 7 | 5g | 4-Chlorophenyl (1h) | 4-Fluorophenyl (2c) | 28 | 43 |
| 8 | 5h | 4-Chlorophenyl (1h) | 4-Tolyl (2h) | 30 | 40 |
| 9 | 5i | 4-Chlorophenyl (1h) | Benzo[d][1,3]dioxol-6-yl (2b) | 30 | 52 |
| 10 | 5j | 4-Fluorophenyl (1i) | Phenyl (2a) | 28 | 49 |
| 11 | 5k | 4-Fluorophenyl (1i) | Benzo[d][1,3]dioxol-6-yl (2b) | 30 | 47 |
| 12 | 5l | 4-Methoxyphenyl (1j) | Phenyl (2a) | 30 | 53 |
a
Reagents and conditions: HOAc (2.0 mL), 100 °C, microwave heating.
b
Isolated yield.