Table 4.
One-pot method for the synthesis of pyrrolo[3,4-b]pyridin-5-one derivatives 1.a
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| Entry | R1 | R | Product | Yield, % |
| 1 | 4-CH3O–C6H4(CH2)2 | Cl | 1a | 60 |
| 2 | H | Cl | 1b | 50 |
| 3 | H | Br | 1c | 60 |
| 4 | H | CH3 | 1d | 59 |
| 5 | CH3 | Cl | 1e | 59 |
| 6 | CH3 | Br | 1f | 70 |
| 7 | CH3 | F | 1g | 54 |
| 8 | CH3 | CH3O | 1h | 55 |
| 9 | CH3 | CH3 | 1i | 68 |
| 10 | HO–(CH2)2 | Cl | 1j | 50 |
aReaction conditions: 1) 2 (3 mmol), amine 3 (9 mmol), AcOH (9 mmol), EtOH, reflux, 4 h. 2) HCl/AcOH, 5 mL/5 mL, reflux, 1 h.
