反应详情

A solution of 6-fluoro-3,4-dihydro-2H-isoquinolin-1-one (300 mg, 1.81 mmol) and potassium carbonate (550 mg, 3.98 mmol) in benzylamine (1.5 ml) was stirred at 180° C. in a microwave for 2 hrs. The solvent was evaporated and the resulting residue partitioned between ethyl acetate (10 ml) and water (10 ml). The organic phase was separated, washed with brine (10 ml), then dried (MgSO4) and evaporated in vacuo. The crude residue was purified by preparative HPLC (Method A) to yield the title compound as a colourless solid (80 mg, 18%). HPLC retention time 3.81 min. Mass spectrum (ES+) m/z 253 (M+H).

1. customThe solvent was evaporated
2. customthe resulting residue partitioned between ethyl acetate (10 ml) and water (10 ml)
3. customThe organic phase was separated
4. washwashed with brine (10 ml)
5. dry with materialdried (MgSO4)
6. customevaporated in vacuo
7. customThe crude residue was purified by preparative HPLC (Method A)