反应详情

温度

80 °C

2N Aqueous NaOH (0.208 mmol) was added to a solution of 5-(5-chloro-1-methyl-6-oxo-1,6-dihydro-pyridin-3-yl)-6-(4-chloro-phenyl)-2-(2,4-dimethoxy-pyrimidin-5-yl)-1-isopropyl-4-oxo-1,4,5,6-tetrahydro-pyrrolo[3,4-b]pyrrole-3-carboxylic acid ethyl ester (Example 220) (0.104 mmol) in 1:1 THF/MeOH (2 mL) and the mixture was stirred at 80° C. for 1 h. After evaporation of MeOH, the pH was adjusted to 5 with addition of 10% w/w aqueous citric acid and extracted with EtOAc (3×). The combined organic phases were successively washed with H2O and brine, dried (Na2SO4), filtered and concentrated. The residue was purified by SFC to afford the title compound as a white solid. tR: 1.10 min (HPLC 3); ESI-MS: tR=0.97 min, [M+H]+ 598/600/602 (LC-MS 1); TLC: Rf=0.31 (9:1 CH2Cl2/MeOH).

1. customAfter evaporation of MeOH
2. additionthe pH was adjusted to 5 with addition of 10% w/w aqueous citric acid
3. extractionextracted with EtOAc (3×)
4. washThe combined organic phases were successively washed with H2O and brine
5. dry with materialdried (Na2SO4)
6. filtrationfiltered
7. concentrationconcentrated
8. customThe residue was purified by SFC