反应详情

Triethylamine (2.60 ml) is added to a solution of (2S)-2-{(3RS)-4-acetyl-3-isopropyl-2-oxo-6-phenyl-1,2,3,4-tetrahydropyrazin-1-yl}methylcarbonylamino-3-phenyl-1-propanol (1.37 g, Compound No. 6-1) in dimethyl sulfoxide (16 ml). A sulfur trioxide-pyridine complex (1.7 g) is added to the mixture, and the whole is stirred overnight. Water is added to the reaction mixture, and the whole is stirred for one hour and extracted with ethyl acetate. The extract is washed with a saturated aqueous ammonium chloride solution, water and saturated brine successively and dried over anhydrous magnesium sulfate. The extract is concentrated under reduced pressure, and the resulting residue is purified by silica gel column chromatography to give the titled compound (631 mg).

1. additionA sulfur trioxide-pyridine complex (1.7 g) is added to the mixture
2. stirringthe whole is stirred for one hour
3. extractionextracted with ethyl acetate
4. washThe extract is washed with a saturated aqueous ammonium chloride solution, water and saturated brine successively
5. dry with materialdried over anhydrous magnesium sulfate
6. concentrationThe extract is concentrated under reduced pressure
7. customthe resulting residue is purified by silica gel column chromatography