反应详情

温度

10 °C

To the solution of rac-(2′S,3′R,4′R,5′R)-6-chloro-4′-(3-chloro-phenyl)-2′-(2,2-dimethyl-propyl)-2-oxo-1,2-dihydro-spiro[indole-3,3′-pyrrolidine]-5′-carboxylic acid (4-cyano-2-methoxy-phenyl)-amide (0.16 g, 0.28 mmol) in DMSO (3 mL) at 0° C. was added an aqueous solution (30% Aldrich) of H2O2 (0.47 g, 4.2 mmol) aqueous solution (1N) of NaOH (1.4 mL, 1.4 mmol) was added dropwise. The reaction mixture was stirred at 10° C. for 1 h. The mixture was partitioned between ethyl acetate and saturated aqueous Na2SO3 solution. The organic layer was separated, washed with water, brine, dried over MgSO4, and concentrated to give rac-(2′S,3′R,4′R,5′R)-6-chloro-4′-(3-chloro-phenyl)-2′-(2,2-dimethyl-propyl)-2-oxo-1,2-dihydro-spiro[indole-3,3′-pyrrolidine]-5′-carboxylic acid (4-carbamoyl-2-methoxy-phenyl)-amide as a white solid (Yield, 0.12 g, 73%)

1. additionwas added dropwise
2. customThe mixture was partitioned between ethyl acetate and saturated aqueous Na2SO3 solution
3. customThe organic layer was separated
4. washwashed with water, brine
5. dry with materialdried over MgSO4
6. concentrationconcentrated
7. customto give