反应详情

To a solution of 1-(4-bromo-phenyl)-3-aza-bicyclo[3.1.0]hexane-3-carboxylic acid tert-butyl ester (Intermediate I, 400 mg, 1.2 mmol) in anhydrous toluene (5 mL) were added Pd2(dba)3 (5.6 mg, 0.006 mmol), BINAP (11.2 mg, 0.018 mmol), sodium tert-butoxide (230 mg, 2.4 mmol) and 3-fluoro-pyrrolidine hydrochloride (170 mg, 1.32 mmol) at r.t. and reaction mixture was refluxed for 3 h. Reaction mixture was then concentrated and the crude product was purified by column chromatography (silica gel, 2:8 EtOAc:Pet. ether) to afford the title compound as viscous liquid (90 mg, 22%).

1. customreaction mixture
2. temperaturewas refluxed for 3 h
3. customReaction mixture
4. concentrationwas then concentrated
5. customthe crude product was purified by column chromatography (silica gel, 2:8 EtOAc:Pet. ether)