COC([N:5]1[CH2:10][CH2:9][CH:8]([C:11]2[C:12]3[CH:19]=[CH:18][C:17]([C:20]([F:23])([F:22])[F:21])=[CH:16][C:13]=3[S:14][CH:15]=2)[CH2:7][CH2:6]1)=O.[BrH:24]>>[BrH:24].[F:23][C:20]([F:21])([F:22])[C:17]1[CH:18]=[CH:19][C:12]2[C:11]([CH:8]3[CH2:7][CH2:6][NH:5][CH2:10][CH2:9]3)=[CH:15][S:14][C:13]=2[CH:16]=1A mixture of 4-(6-trifluoromethyl-benzo[b]thiophen-3-yl)-piperidine-1-carboxylic acid methyl ester (3.1 g, 9.0 mmol) in HBr (45 mL, 30% in acetic acid) was stirred at room temperature for 20 hours wher the volatiles were removed in vacuo. The residue was washed with EtOAc and the product was collected by filtration yielding 3.09 g (94%) of the desired product as a white solid.
読み込み中…