Trifluoroacetic acid → HCID 66846903、化合物

反応式

C(O)(C(F)(F)F)=O.[Br:8][C:9]1[S:10][C:11]([NH:23]C(=O)OC(C)(C)C)=[C:12]([C:14]2[CH:19]=[C:18]([Cl:20])[CH:17]=[CH:16][C:15]=2[O:21][CH3:22])[N:13]=1>C(Cl)Cl.O>[Br:8][C:9]1[S:10][C:11]([NH2:23])=[C:12]([C:14]2[CH:19]=[C:18]([Cl:20])[CH:17]=[CH:16][C:15]=2[O:21][CH3:22])[N:13]=1

参加物

実験手順

TFA (4.0 mL) was added to a solution of tert-butyl 2-bromo-4-(5-chloro-2-methoxyphenyl)thiazol-5-ylcarbamate (360 mg, 0.86 mmol) in DCM (10 mL) and water (3 drops). The reaction mixture was stirred for 1.5 hours at room temperature and then evaporated to dryness. The residue was taken up into DCM and washed with sodium hydrogen carbonate (sat.aq.), water and brine, and concentrated under vacuum to give 2-bromo-4-(5-chloro-2-methoxyphenyl)thiazol-5-amine as an orange residue. LCMS (method 1) [M+H]+=321.3, RT=3.63 min. 1H NMR (400 MHz, DMSO-d6): δ (ppm) 7.36 (d, 1H), 7.34-7.32 (m, 1H), 7.10 (d, 1H), 3.83 (s, 3H).