反应详情

TFA (32.4 mmol) was added to a solution of 4-[6-(4-chloro-phenyl)-2-(2,4-dimethoxy-pyrimidin-5-yl)-1-isopropyl-4-oxo-4,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-5-yl]-piperidine-1-carboxylic acid tert-butyl ester (Step I06.1) (0.755 mmol) in CH2Cl2 (4 mL) at 0° C. After 1 h, the reaction mixture was quenched with a saturated aqueous solution of NaHCO3 and diluted with EtOAc, THF and NaCl. The separated aqueous phase was extracted with EtOAc/THF (2×). The combined organic phases were dried (MgSO4), filtered and concentrated. The residue was purified using a RediSep® silica gel column to afford the title compound as a white solid (TFA-salt). tR: 4.34 min (HPLC 4); ESI-MS: tR=0.82 min, [M+H]+ 496/498(LC-MS 1).

1. customthe reaction mixture was quenched with a saturated aqueous solution of NaHCO3
2. additiondiluted with EtOAc, THF and NaCl
3. extractionThe separated aqueous phase was extracted with EtOAc/THF (2×)
4. dry with materialThe combined organic phases were dried (MgSO4)
5. filtrationfiltered
6. concentrationconcentrated
7. customThe residue was purified