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0 °C

Under Ar, (S)-(2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine-6-amine (110 mg, 0.6 mmol) was dissolved in DMF (6 mL), cooled to 0° C., added Et3N (0.21 mL, 2 mmol), added 3-(4-(4-(trifluoromethoxy)phenoxy)piperidin-1-yl) propionyl chloride (291 mg, 0.75 mmol) in batches, naturally rose to room temperature and stirred for 3 h, added an appropriate amount of dichloromethane, washed by distilled water for 3 times, followed by anhydrous sodium sulphate drying, filtrated out drying agent and spinning dry, residuals were purified by column chromatography (eluent CH2Cl2: MeOH=30:1) to give 70 mg target product, yield was 23%.

1. customnaturally rose to room temperature
2. washwashed
3. distillationby distilled water for 3 times
4. filtrationfiltrated
5. customout drying agent
6. customspinning dry
7. customresiduals were purified by column chromatography (eluent CH2Cl2: MeOH=30:1)
8. customto give 70 mg target product, yield was 23%