反应详情

(R)—N2-Indan-1-yl-quinoline-2,5-diamine (200 mg, 0.73 mmol) was dissolved in 2 mL pyridine and cyclopropane sulfonylchloride (102 mg, 0.73 mmol) was added. The reaction mixture was stirred at room temperature overnight and quenched by addition of 50 mL water and acetic acid until pH 5. 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 (cyclohexane/ethyl acetate 100:0→50:50 gradient). The title compound was obtained as a brown solid (160 mg, 58%), MS: m/e=380.4 (M+H+).

1. customquenched by addition of 50 mL water and acetic acid until pH 5
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 (cyclohexane/ethyl acetate 100:0→50:50 gradient)