反应详情

N-{5-[(1R)-1-{[tert-butyl(dimethyl)silyl]oxy}-2-({2-[4-(3-{3-[(1R)-3-(diisopropylamino)-1-phenylpropyl]-4-hydroxyphenyl}propoxy)phenyl]ethyl}amino)ethyl]-2-hydroxyphenyl}methanesulfonamide (Preparation 10, 98 mg, 0.11 mmol) was dissolved in tetrahydrofuran (4 ml) and methanol (2 ml) and triethylaminetrihydrofluoride (95 ul, 0.58 mmol) was added in one portion at room temperature. The reaction was stirred for 24 hours and the solvent removed under reduced pressure, the residue was dissolved in methanol (10 ml) and 880 ammonia (1 ml) and the solvent removed under reduced pressure to yield an off white solid. The solid was dissolved in methanol (1 ml) and precipitated with an excess of diisopropylether, the solid was collected by filtration to furnish the title compound as a white solid, 16 mg.

1. customthe solvent removed under reduced pressure
2. dissolutionthe residue was dissolved in methanol (10 ml)
3. custom880 ammonia (1 ml) and the solvent removed under reduced pressure
4. customto yield an off white solid
5. customprecipitated with an excess of diisopropylether
6. filtrationthe solid was collected by filtration