Trifluoroacetic acid → 3-[Cyclopropyl(4-fluorophenyl)methyl]-7-[(methylsulfanyl)methyl]-1H-indole

反応式

[CH:1]1([CH:4]([C:6]2[CH:11]=[CH:10][C:9]([F:12])=[CH:8][CH:7]=2)O)[CH2:3][CH2:2]1.FC(F)(F)C(O)=O.[CH3:20][S:21][CH2:22][C:23]1[CH:24]=[CH:25][CH:26]=[C:27]2[C:31]=1[NH:30][CH:29]=[CH:28]2>ClCCl>[CH:1]1([CH:4]([C:6]2[CH:11]=[CH:10][C:9]([F:12])=[CH:8][CH:7]=2)[C:28]2[C:27]3[C:31](=[C:23]([CH2:22][S:21][CH3:20])[CH:24]=[CH:25][CH:26]=3)[NH:30][CH:29]=2)[CH2:3][CH2:2]1

参加物

実験手順

188 mg (1.13 mmol) of cyclopropyl(4-fluorophenyl)methanol and 0.10 ml (1.35 mmol) of trifluoroacetic acid were added to 200 mg (1.13 mmol) of the compound from Example 8A in 13 ml of dichloromethane. The reaction mixture was stirred at RT for 15 min, the solvent was removed in vacuo, and the crude product was then purified by preparative HPLC (mobile phase: acetonitrile/water gradient). 267 mg (73% of theory) of the title compound were obtained.