反应详情

A solution of 2-(4-((4-(4-amino-3-fluorobenzyl)piperidin-1-yl)methyl)phenyl)-1,1,1,3,3,3-hexafluoropropan-2-ol (0.861 mmol, 0.4 g) and 4-nitrophenyl carbonochloridate (0.861 mmol, 0.174 g) in tetrahydrofuran (5 mL) was stirred at room temperature for 30 minutes. 2-Methylpropane-1,2-diamine (1.723 mmol, 0.152 g) was added, followed by triethylamine (2.58 mmol, 0.360 mL, 0.261 g) and the reaction stirred at room temperature overnight. The reaction mixture was concentrated under vacuum. The residue was purified by prep-HPLC (acidic conditions) and SCX chromatography to afford the title compound (45.3 mg). MS (ESI) m/z 579.2 [M+H]+

1. concentrationThe reaction mixture was concentrated under vacuum
2. customThe residue was purified by prep-HPLC (acidic conditions) and SCX chromatography