反应详情

To a solution of (R)-4-(piperidin-3-ylmethoxy)-9-((2-(trimethylsilyl)ethoxy)methyl)-9H-dipyrido[2,3-b;4′,3′-d]pyrrole-6-carbonitrile (50 mg, 0.1 mmol) in acetonitrile (0.5 mL) and water (0.1 mL) was added Formalin (0.024 mL, 0.3 mmol) followed by sodium triacetoxyborohydride (48 mg, 0.2 mmol). The reaction mixture was stirred for 20 minutes at ambient temperature and then basified by the addition of saturated aqueous sodium carbonate solution (1 mL), diluted with methylene chloride (50 mL) and methanol (5 mL), and washed with saturated aqueous sodium bicarbonate solution (2×15 mL). The organic layer was separated, dried over sodium sulfate, and concentrated in vacuo to afford a pale yellow solid, which was used in the next step without any further purification (45 mg).

1. washwashed with saturated aqueous sodium bicarbonate solution (2×15 mL)
2. customThe organic layer was separated
3. dry with materialdried over sodium sulfate
4. concentrationconcentrated in vacuo
5. customto afford a pale yellow solid, which
6. customwas used in the next step without any further purification (45 mg)