反应详情

5-[(1R)-2-(Benzylamino)-1-hydroxyethyl]-8-(benzyloxy)quinolin-2(1H)-one (40 mg) was dissolved in MeCN (2 ml). N,N,-diisopropylethylamine (0.03 ml) and 1-{4-[(6-bromohexyl)oxy]butyl}-3-(cyclopentylsulfonyl)benzene (Example 1v) (30 mg) were added and the reaction mixture was heated at 80° under nitrogen for 48 h. The mixture was then diluted with water and extracted with EtOAc. The organic phases were combined, dried (MgSO4), and evaporated in vacuo. The residue was purified on a silica SPE bond elut cartridge, eluting with EtOAc-cyclohexane mixtures, to give the title compound, (13 mg)

1. temperaturethe reaction mixture was heated at 80° under nitrogen for 48 h
2. extractionextracted with EtOAc
3. dry with materialdried (MgSO4)
4. customevaporated in vacuo
5. customThe residue was purified on a silica SPE bond elut cartridge
6. washeluting with EtOAc-cyclohexane mixtures