反应详情

Mono-tert-butyl 3-{4-cyclopropyl-5-[3-(2-ethylbutyl)cyclobutyl]isoxazol-3-yl}glutarate (150 mg) and DMF (1.5 mL) were mixed. To the mixture were added HOBt.H2O (63.5 mg), WSC.HCl (79.6 mg) and 2-chloro-4-methylphenylamine (0.0512 mL). The mixture was stirred at RT overnight. To the reaction mixture was added ethyl acetate. The mixture was washed with aqueous 10 w/v % citric acid, water, saturated aqueous sodium bicarbonate and brine, then dried over sodium sulfate. The sodium sulfate was filtered off and the filtrate was concentrated in vacuo. The resultant residue was purified by preparative chromatography (Eluent: ethyl acetate/hexane=1/6) to give the title compound (122 mg).

1. washThe mixture was washed with aqueous 10 w/v % citric acid, water, saturated aqueous sodium bicarbonate and brine
2. dry with materialdried over sodium sulfate
3. filtrationThe sodium sulfate was filtered off
4. concentrationthe filtrate was concentrated in vacuo
5. customThe resultant residue was purified by preparative chromatography (Eluent: ethyl acetate/hexane=1/6)