反应详情

A solution of 3-(4-fluorophenyl)-3-(3-trifluoromethyl-benzenesulfonylamino)-propionic acid (172 mg, 0.44 mmol), crude 2-(5-amino-5,6,7,8-tetrahydro-quinazolin-2-yl)-ethanol (Step G, 85 mg, 0.44 mmol), HOBt (65.5 mg, 0.484 mmol) and EDC (93 mg, 0.484 mmol) in 1.5 mL of DMF was stirred overnight at RT. After quenching with Sat. NaHCO3 solution, the mixture was extracted with EtOAc. The combined organic phase was washed brine, dried over Na2SO4, and evaporated in vacuo. Flash chromatography (SiO2, EtOAc/MeOH=100:5 to 100:10 to 100:12) gave the title compound as a white solid. MS: 567.0 (M+1).

1. customAfter quenching with Sat. NaHCO3 solution
2. extractionthe mixture was extracted with EtOAc
3. washThe combined organic phase was washed brine
4. dry with materialdried over Na2SO4
5. customevaporated in vacuo