反应详情

(2S,4S)-1-[[N-(4-Carboxybicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile (30.0 mg), along with 1-hydroxybenzotriazole, was dissolved in N,N-dimethylformamide (1.0 mL). To this solution, 2-aminothiazole (18.6 mg) and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (53.4 mg) were added, and the mixture was stirred at room temperature for 15 hours. The solvent was evaporated under reduced pressure and the resulting residue was purified by preparative thin-layer chromatography (solvent:dichloromethane:methanol=9:1) to give (2S,4S)-4-fluoro-1-[[N-[4-[N-(thiazol-2-yl)amino]carbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]pyrrolidine-2-carbonitrile (17.4 mg).

1. customThe solvent was evaporated under reduced pressure
2. customthe resulting residue was purified by preparative thin-layer chromatography (solvent:dichloromethane:methanol=9:1)