反应详情

To a 50 mL round-bottomed flask was added (R)—N-(2-(1,3-dioxoisoindolin-2-yl)ethyl)-N-(4-fluorophenyl)-1-(4-(trifluoromethyl)phenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide (16 mg, 27 μmol, from step 4), EtOH (1 mL), hydrazine, anhydrous (3.5 μL, 109 μmol, Aldrich). The solution was stirred at RT for 18 h. The solvent was removed in vacuo and the residue was purified by silica gel chromatography, eluting with 10% MeOH/CH2Cl2+1% ammonia (37% in water) to give (R)—N-(2-aminoethyl)-N-(4-fluorophenyl)-1-(4-(trifluoromethyl)-phenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide. MS (ESI pos. ion) m/z: 458 (M+1).

1. customThe solvent was removed in vacuo
2. customthe residue was purified by silica gel chromatography
3. washeluting with 10% MeOH/CH2Cl2+1% ammonia (37% in water)