反应详情

Treat a solution of 1-(5-amino-2-bromo-4-fluorophenyl)propan-2-one (5 g, 27.62 mmol) and 4-amino-2-methylsulfanyl-pyrimidine-5-carbaldehyde (4.67 g, 27.62 mmol) in EtOH (30 mL) with sodium ethoxide (3.76 g, 55.25 mmol) and stir at RT for 12 h. Concentrate the mixture to dryness, treat with water, extract with EtOAc (3×), wash the combined organics with brine, dry with Na2SO4, concentrate and purify by silica gel chromatography (EtOAc/Pet Ether, 1:4) to afford the title compound (1.7 g, 16% yield). MS (m/z): 379.1/381.1 (M+1).

1. concentrationConcentrate the mixture to dryness
2. additiontreat with water
3. extractionextract with EtOAc (3×)
4. washwash the combined organics with brine
5. dry with materialdry with Na2SO4
6. concentrationconcentrate
7. custompurify by silica gel chromatography (EtOAc/Pet Ether, 1:4)