Trifluoroacetic acid → 5-(4-(aminomethyl)-2-fluorophenyl)-1-methylpyridin-2(1H)-one
Reaction equation
[F:1][C:2]1[CH:3]=[C:4]([CH:14]=[CH:15][C:16]=1[C:17]1[CH:22]=[CH:21][C:20](=[O:23])[N:19]([CH3:24])[CH:18]=1)[CH2:5][NH:6]C(=O)OC(C)(C)C.FC(F)(F)C(O)=O>ClCCl>[NH2:6][CH2:5][C:4]1[CH:14]=[CH:15][C:16]([C:17]2[CH:22]=[CH:21][C:20](=[O:23])[N:19]([CH3:24])[CH:18]=2)=[C:2]([F:1])[CH:3]=1Participants
4
Procedure
The crude tert-butyl 3-fluoro-4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)benzylcarbamate 21-6 (10 mg, obtained in Step 3) was stirred with trifluoroacetic acid (TFA, 0.3 mL) in dichloromethane (1 mL) overnight. Evaporation under reduced pressure (with the addition of some toluene to aid evaporation of the residual TFA) followed by lyophilization gave the crude 5-(4-(aminomethyl)-2-fluorophenyl)-1-methylpyridin-2(1H)-one 21-7.