Cyclobutylamine → tert-Butyl 4-(4-(3-cyclobutylureido)-3-fluorobenzoyl)piperazine-1-carboxylate

Participants

Reaction Steps

tert-Buty 4-(4-amino-3-fluorobenzoyl)piperazine-1-carboxylate (9.5 g, 29.41 mmol) was dissolved in dichloromethane (100 mL) and 4-nitrophenyl carbonochloridate (5.93 g, 29.41 mmol) was added. The reaction mixture was stirred for 20 hours and cyclobutylamine (7.5 mL, 88.2 mmol) added. After 2 hours, the reaction mixture was chromatographed on silica (eluting with dichloromethane to dichloro-methane/ethyl acetate) to give the title compound (2.8 g). MS (ESI) m/z: 421.0 [M+H]+

Provenance & Evidence