反应详情

A solution of intermediate 6 (200 mg, 0.400 mmol), quinoline-2-carbaldehyde (251 mg, 1.600 mmol), triethylamine (61 mL, 0.440 mmol) and formic acid (263 μL, 3.20 mmol), in acetonitrile (4 ml) is irradiated with microwaves (130° C., 20 minutes). The reaction mixture was partitioned between AcOEt and 5% NaHCO3 solution. The organic layers were then washed with brine, dried over Na2SO4 and filtered. The solvent was evaporated and the crude was purified by silica gel chromatography (DCM/MeOH 99:1) to give compound 11 (132 mg, 54.6% yield).

1. customThe reaction mixture was partitioned between AcOEt and 5% NaHCO3 solution
2. washThe organic layers were then washed with brine
3. dry with materialdried over Na2SO4
4. filtrationfiltered
5. customThe solvent was evaporated
6. customthe crude was purified by silica gel chromatography (DCM/MeOH 99:1)