反应详情

At 0° C., 0.8 ml of TFA was added to a solution of 119 mg (0.40 mmol) of tert-butyl [4-(5-thioxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]carbamate in 4 ml of dichlormethane, and the mixture was stirred at RT for 40 min. Subsequently, the reaction mixture was concentrated under reduced pressure. Ethyl acetate and a saturated aqueous sodium bicarbonate solution were added to the residue. After phase separation, the aqueous phase was extracted with ethyl acetate. The aqueous phase was concentrated and the crude product was purified by preparative HPLC (water/acetonitrile/0.1% formic acid gradient). Yield: 30 mg (38% of theory)

1. concentrationSubsequently, the reaction mixture was concentrated under reduced pressure
2. additionEthyl acetate and a saturated aqueous sodium bicarbonate solution were added to the residue
3. customAfter phase separation
4. extractionthe aqueous phase was extracted with ethyl acetate
5. concentrationThe aqueous phase was concentrated
6. customthe crude product was purified by preparative HPLC (water/acetonitrile/0.1% formic acid gradient)