反应详情

温度

45 °C

(R)—N2-Indan-1-yl-quinoline-2,5-diamine (example 43, step A+B, 200 mg, 0.727 mmol) was dissolved in 3 mL pyridine and 4-fluoro-phenylsulfamoyl chloride (298 mg, 1.42 mmol) was added. The reaction mixture was stirred at 45° C. for 2 days and quenched by addition of 50 mL water. The mixture was extracted three times with ethyl acetate (50 mL each). The organic phases ware pooled, dried with sodium sulfate, filtered and evaporated. The residue was purified by flash chromatography on silica gel (heptane, tetrahydrofurane 100:0->50:50 gradient). The title compound was obtained as a brown solid (43 mg, 13%), MS: m/e=449.1 (M+H+).

1. customquenched by addition of 50 mL water
2. extractionThe mixture was extracted three times with ethyl acetate (50 mL each)
3. dry with materialdried with sodium sulfate
4. filtrationfiltered
5. customevaporated
6. customThe residue was purified by flash chromatography on silica gel (heptane, tetrahydrofurane 100:0->50:50 gradient)