{(S)-1-[4-Fluoro-2-(6-fluoropyridin-3-ylamino)phenylcarbamoyl]ethyl}carbamic acid tert-butyl ester → (S)-2-Amino-N-[4-fluoro-2-(6-fluoropyridin-3-ylamino)phenyl]propionamide

Participants

Reaction Steps

A mixture of {(S)-1-[4-fluoro-2-(6-fluoropyridin-3-ylamino)phenylcarbamoyl]ethyl}carbamic acid tert-butyl ester (276 mg, 0.70 mmol) in DCM (1 mL) and TFA (1 mL) was stirred at RT for 3 h. The reaction mixture was loaded onto an Isolute® SCX-2 cartridge then washed with MeOH followed by 2M NH3/MeOH. The basic fractions were combined and concentrated in vacuo to afford the title compound as a yellow oil (193 mg, 94%). LCMS (Method C): RT 0.29 and 1.93 min [M+H]+ 293.2.

Provenance & Evidence