反应详情

To a mixture of 3-{3-amino-4-[4-(3,5-dimethylpyridin-2-yl)piperazine-1-carbonyl]phenyl}oxazolidin-2-one (93.1 mg) described in Example 133, triethylamine (63 μL) and tetrahydrofuran (1 mL) was added 3-chloropropanesulfonyl chloride (38 μL), and the mixture was stirred overnight. Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine, and the solvent was evaporated. To the residue were added 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) (42 μL) and DMF (1 mL), and the mixture was stirred at room temperature. Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine, and the solvent was evaporated. To the residue was added a mixed solvent of isopropyl ether and ethyl acetate, and the precipitated crystals were collected by filtration to give the title compound (62.1 mg).

1. extractionthe mixture was extracted with ethyl acetate
2. washThe organic layer was washed with saturated brine
3. customthe solvent was evaporated
4. additionTo the residue were added 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) (42 μL) and DMF (1 mL)
5. stirringthe mixture was stirred at room temperature
6. additionWater was added to the reaction mixture
7. extractionthe mixture was extracted with ethyl acetate
8. washThe organic layer was washed with saturated brine
9. customthe solvent was evaporated
10. additionTo the residue was added a mixed solvent of isopropyl ether and ethyl acetate
11. filtrationthe precipitated crystals were collected by filtration