反应详情

(2R)-2-(2-Amino-2-methylpropanamido)-4-methyl-N-[2-oxo-8-(2-oxopyrrolidin-1-yl)-1-(thiophen-3-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]pentanamide (1.08 g) was dissolved in acetic acid (30 mL), and a solution of L-(+)-ascorbic acid (3.52 g) and Cu(ClO4)2.6H2O (741 mg) in water (40 mL) was added thereto, followed by stirring at room temperature for 15 minutes while oxygen gas was bubbled into the mixture. Saturated aqueous sodium chloride solution was added to the reaction mixture, and the mixture was washed with ethyl acetate twice. Sodium bicarbonate (88.2 g) was added to the aqueous layer, and the mixture was extracted with chloroform twice. The organic layer was concentrated under reduced pressure, and the thus-recovered residue was purified through chromatography, whereby the title compound (0.5 mg) was yielded.

1. customwas bubbled into the mixture
2. additionSaturated aqueous sodium chloride solution was added to the reaction mixture
3. washthe mixture was washed with ethyl acetate twice
4. additionSodium bicarbonate (88.2 g) was added to the aqueous layer
5. extractionthe mixture was extracted with chloroform twice
6. concentrationThe organic layer was concentrated under reduced pressure
7. customthe thus-recovered residue was purified through chromatography, whereby the title compound (0.5 mg)
8. customwas yielded