反应详情

(3R)-3-[5-{2-[4-(2-aminoethyl)phenoxy]ethyl}-2-(benzyloxy)phenyl]-N,N-diisopropyl-3-phenylpropan-1-amine (Preparation 21, 95 mg, 0.17 mmol), N-{2-(benzyloxy)-5-[(1R)-2-bromo-1-{[tert-butyl(dimethyl)silyl]oxy}ethyl]phenyl}methanesulfonamide (WO2005/080324, 86 mg, 0.17 mmol), sodium hydrogen carbonate (42 mg, 0.51 mmol) and potassium iodide (28 mg, 0.17 mmol) were added to acetonitrile (2.5 ml) and heated to reflux for 24 hours, then cooled to room temperature and the solvents removed in vacuo, the residue was purified by column chromatography on silica gel eluting with dichloromethane:methanol:880 ammonia (2421810.8 to 95/5/0.5 by volume) to furnish the title compound as a white foam, 78 mg.

1. temperatureheated
2. temperatureto reflux for 24 hours
3. customthe solvents removed in vacuo
4. customthe residue was purified by column chromatography on silica gel eluting with dichloromethane