反应详情

Combine N-{3-[5-fluoro-1-(3-iodo-propyl)-indan-1-yl]-1H-indol-7-yl}-methane sulfonamide (65 mg, 0.13 mmol) and morpholine (2 ml) in anhydrous tetrahydrofuran (2.5 ml) and stir at room temperature under nitrogen overnight. Remove the volatiles under high vacuum, dissolve the residue in dichloromethane, add solid potassium carbonate, stir for ten minutes, filter, and concentrate in vacuo. Purify the residue on silica eluting with 5 to 10% methanol in dichloromethane over 15 minutes to obtain the title compound as a white solid (50 mg, 83%). LC-MS m/z 472.2 (M++1).

1. customRemove the volatiles under high vacuum
2. dissolutiondissolve the residue in dichloromethane
3. additionadd solid potassium carbonate
4. filtrationfilter
5. concentrationconcentrate in vacuo
6. customPurify the residue on silica eluting with 5 to 10% methanol in dichloromethane over 15 minutes