abstract |
The invention discloses a synthetic rivaroxaban key intermediate (S)-2-{[2-oxo-3-(4-(3-oxomorpholine)phenyl)oxazolidin-5-yl]methanol Base} isoindole-1,3-dione method, combining 4-(4-carbaaminophenyl)-3-morpholinone with (S)-{1-(chloroformate group)- 2-[2-(1,3-dioxoisoindol) base] ethyl} halide salt can be obtained by ring-closing reaction. The method is easy to operate, the raw materials are readily available, and the yield can be as high as about 90%. The prepared (S)-2-{[2-oxo-3-(4-(3-oxomorpholine)phenyl)oxazolidine -5-yl]methyl}isoindole-1,3-dione has good purity, the purity can be as high as more than 98%, and is suitable for large-scale industrial production. |