反应详情

温度

0 °C

(S)-N-[3-(3-fluoro-4-morpholinylphenyl)-2-oxo-5-oxazolidinyl]methyl amine (0.200 gm, 0.00068 moles) was taken up in 1:1 THF-water mixture (20 ml). To this was added 4-oxo-4 (2-thienyl)butanoic acid (0.125 gm, 0.00068 moles) and HOBt (0.091 gm, 0.00068 moles). The resulting mixture was cooled to 0° C. and then 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (0.142 gm, 0.00074 moles) was added and the resulting mixture was allowed to warm to room temp and then stirred for 24 hr. The reaction mixture was concentrated, 15 ml of saturated sodium bicarbonate was added, stirred for 15 min and then extracted with ethyl acetate. The ethyl acetate layer was separated and the solvent evaporated off. The residue was chromatographed over silica gel (100-200 mesh, 20 gm). The column was eluted with mixture of ethyl acetate:hexane, and finally with ethyl acetate. The combined fractions were concentrated to give the title compound (0.175 gm, 56%) as a white solid.

1. temperatureto warm to room temp
2. concentrationThe reaction mixture was concentrated
3. addition15 ml of saturated sodium bicarbonate was added
4. stirringstirred for 15 min
5. extractionextracted with ethyl acetate
6. customThe ethyl acetate layer was separated
7. customthe solvent evaporated off
8. customThe residue was chromatographed over silica gel (100-200 mesh, 20 gm)
9. washThe column was eluted with mixture of ethyl acetate
10. concentrationThe combined fractions were concentrated