反应详情

A solution of 5-(2-bromo-5-(trifluoromethyl)phenyl)-1,2,3,4-tetrahydroisoquinoline hydrochloride (Intermediate T, 0.200 g, 0.509 mmol), N-(5-fluorothiazol-2-yl)-1H-imidazole-1-sulfonamide (Intermediate N, 0.506 g, 2.037 mmol), and triethylamine (1.420 ml, 10.19 mmol) in 3 mL THF was heated to 80° C. for 30 minutes. The reaction mixture was diluted with EtOAc and washed with 1N citric acid. The organics were dried over MgSO4 and concentrated. Purification of the resulting residue by silica gel column chromatography (0 to 100% EtOAc/heptane) gave 5-(2-bromo-5-(trifluoromethyl)phenyl)-N-(5-fluorothiazol-2-yl)-3,4-dihydroisoquinoline-2(1H)-sulfonamide (0.104 g, 0.194 mmol).

1. washwashed with 1N citric acid
2. dry with materialThe organics were dried over MgSO4
3. concentrationconcentrated
4. customPurification of the resulting residue by silica gel column chromatography (0 to 100% EtOAc/heptane)