反应详情

Triethylamine (90 μL, 0.65 mmol) was added to a solution of (1-(10-oxodecyl)piperidin-4-yl)methyl 2-cyclohexyl-2-hydroxy-2-phenylacetate (182 mg, 0.39 mmol) and (R)-5-(2-amino-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one hydrochloride (100 mg, 0.39 mmol) in methanol (4 mL). The reaction mixture was stirred at RT for 1 hour. Sodium triacetoxyborohydride (154 mg, 0.73 mmol) followed by acetic acid (74 μL, 1.29 mmol) were added, and the reaction mixture stirred at RT for 72 hours. The reaction was quenched with water (500 μL) and evaporated under reduced pressure. The residue was dissolved in dimethyl sulfoxide and submitted to reverse phase preparative HPLC for final purification. The title compound was isolated (42.3 mg, 16%).

1. additionwere added
2. stirringthe reaction mixture stirred at RT for 72 hours
3. customThe reaction was quenched with water (500 μL)
4. customevaporated under reduced pressure
5. dissolutionThe residue was dissolved in dimethyl sulfoxide
6. custompurification