反应详情

(±)-3-(Methanesulfonyl-{6-[1-(3-trifluoromethyl-phenylcarbamoyl)-1H-indol-5-yloxy]-pyrimidin-4-ylmethyl}-amino)-pyrrolidine-1-carboxylic acid tert-butyl ester (12 mg, 0.018 mmol) is stirred in a solution of DCM (2 mL) and TFA (0.5 mL) overnight. After removal of solvents, the residue is quenched with saturated aqueous sodium bicarbonate. The mixture is extracted with EtOAc (3×). The combined organic layers are washed with water and brine and the organic layer is dried with Na2SO4, filtered, and condensed. The residue is then separated by FCC (0-10%, 2 M NH3 in MeOH/DCM) to provide the title compound. MS (ESI) m/z 574.8 (M+1).

1. customAfter removal of solvents
2. customthe residue is quenched with saturated aqueous sodium bicarbonate
3. extractionThe mixture is extracted with EtOAc (3×)
4. washThe combined organic layers are washed with water and brine
5. dry with materialthe organic layer is dried with Na2SO4
6. filtrationfiltered
7. customcondensed
8. customThe residue is then separated by FCC (0-10%, 2 M NH3 in MeOH/DCM)