Trifluoroacetic acid → 5-(3-(ethylsulfonyl)phenyl)-8-methoxy-N,3-dimethyl-9H-pyrido[2,3-b]indol-7-amine

Participants

Reaction Steps

The crude residue from previous step (Compound 251) was dissolved in 3 mL CH2Cl2 and to were sequentially added 0.2 mL of anisole and 1 mL of TFA. The mixture was stirred at room temperature for 2 h. Solvent was removed in vacuum and the residue was basified with saturated aqueous NaHCO3 and extracted with EtOAc. The organic layer was washed with brine, dried over Na2SO4 and finally purified flash chromatography to furnish Compound 252 (287 mg, 70%, for 2 steps).

Provenance & Evidence