Tetrahydrofuran → HCID 86670950, compound

Participants

Reaction Steps

A solution of 2-(4-((4-(4-amino-2-chloro-5-fluorobenzyl)piperidin-1-yl)methyl)phenyl)-1,1,1,3,3,3-hexafluoropropan-2-ol (0.200 mmol, 100 mg) and 4-nitrophenyl carbonochloridate (0.200 mmol, 40.4 mg) in tetrahydrofuran (5 mL) was stirred at room temperature for 30 minutes. 1-Amino-2-methylpropan-2-ol (0.401 mmol, 0.051 mL, 35.7 mg) was added and the reaction was kept at room temperature overnight. The reaction mixture was concentrated under vacuum and residue purified by silica column chromatography (eluent: dichloromethane-5% methanol in dichloromethane) to afford the title compound (58.5 mg). MS (ESI) m/z 614.1 [M+H]+

Provenance & Evidence