反应详情

温度

80 °C

The suspension of 5-(4-ethoxy-quinolin-6-ylmethylene)-2-methylsulfanyl-thiazol-4-one (example 40b) (100 mg, 0.3 mmol), m-fluorophenylethylamine (80 ul, 0.6 mmol) and DIEA (0.10 mL, 0.6 mmol) in acetoniltile (2 mL) was stirred under at 80° C. for 3 h. After cooling to room temperature, the solid was collected by filtration, washed with a little bit of acetonitrile and dried. Flash chromatography (Merck Silica gel 60, 230-400 mesh, 0%-5% methanol in methylene chloride in 30 min) afforded 5-(4-ethoxy-quinolin-6-ylmethylene)-2-[2-(3-fluoro-phenyl)-ethylamino]-thiazol-4-one (90 mg, 70%) as a light yellow solid: LC-MS m/e 422 (MH+).

1. temperatureAfter cooling to room temperature
2. filtrationthe solid was collected by filtration
3. washwashed with a little bit of acetonitrile
4. customdried