反应详情

(2S,4S)-1-[[N-Benzyloxycarbonyl-N-(4-carboxybicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile (91.5 mg) and 1-hydroxybenzotriazole (45.9 mg) were dissolved in N,N-dimethylformamide (2.0 mL). While the solution was chilled in an ice bath, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (95.9 mg) was added and the mixture was allowed to warm to room temperature and was stirred for 15 hours. The solvent was evaporated under reduced pressure and the residue was purified by silica gel chromatography (eluant:ethyl acetate) to give (2S,4S)-1-[[N-benzyloxycarbonyl-N-[4-(benzotriazol-1-yl)oxycarbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile (92.0 mg).

1. temperatureWhile the solution was chilled in an ice bath
2. customThe solvent was evaporated under reduced pressure
3. customthe residue was purified by silica gel chromatography (eluant:ethyl acetate)