反应详情

N-{5-[(1R)-1-{[tert-butyl(dimethyl)silyl]oxy}-2-({2-[4-(4-{3-[(1R)-3-(diisopropylamino)-1-phenylpropyl]-4-hydroxyphenyl}butoxy)phenyl]ethyl}amino)ethyl]-2-hydroxyphenyl}methanesulfonamide (Preparation 15, 190 mg, 0.22 mmol) was dissolved in tetrahydrofuran (5 ml) and N,N-diethylethanamine trihydrofluoride (0.2 ml, 1 mmol) was added dropwise. After 29 hours a mixture of tetrahydrofuran (5 ml) and 880 ammonia (5 ml) were added and after 15 minutes brine was added, the organic layer was separated, dried (magnesium sulphate), filtered, the solvents were removed in vacuo and the residue was purified by column chromatography on silica gel eluting with dichloromethane:methanol:880 ammonia (981210.2 to 92/8/0.8 by volume) to furnish the title compound as a white foam, 90 mg.

1. additionwas added
2. customthe organic layer was separated
3. dry with materialdried (magnesium sulphate)
4. filtrationfiltered
5. customthe solvents were removed in vacuo
6. customthe residue was purified by column chromatography on silica gel eluting with dichloromethane