反应详情

2-(3-Fluoro-4-(5-(1-phenylcyclopropyl)thiazolo[5,4-b]pyridin-2-yl)phenyl)acetaldehyde (44 mg, 0.113 mmol) was dissolved in chloroform (1.1 mL) before it was stirred at ambient temperature with benzylamine (62 μl, 0.57 mmol) and PTSA (1 mg) for 16 h. Methanol (1.1 mL) and sodium cyanoborohydride (7.1 mg, 0.113 mmol) were then added and allowed to stir in the reaction mixture over 3 d. The reaction mixture was diluted with DCM, added to a separatory funnel, partitioned with sodium bicarbonate (saturated, aqueous), washed with sodium bicarbonate (saturated, aqueous), separated, dried over sodium sulfate, and concentrated via rotovap to give the title compound after flash chromatography. MS (ESI) m/z: Calculated: 479.2; Observed: 480.1 (M++H).

1. additionadded to a separatory funnel
2. custompartitioned with sodium bicarbonate (saturated, aqueous)
3. washwashed with sodium bicarbonate (saturated, aqueous)
4. customseparated
5. dry with materialdried over sodium sulfate
6. concentrationconcentrated via rotovap