[Cl:1][C:2]1[CH:3]=[C:4]([NH:9][C:10](=[O:31])[CH2:11][N:12]2[CH:16]=[C:15]([C:17]3[CH:22]=[CH:21][C:20]([N:23]4[CH:27]=[C:26]([CH3:28])[N:25]=[CH:24]4)=[C:19]([O:29][CH3:30])[CH:18]=3)[N:14]=[N:13]2)[CH:5]=[CH:6][C:7]=1[F:8].C[Si]([N-][Si](C)(C)C)(C)C.[K+].[O:42]([CH2:50][C:51]([F:54])([F:53])[F:52])S(C(F)(F)F)(=O)=O>CN(C=O)C>[F:52][C:51]([F:54])([F:53])[C:50]([OH:29])=[O:42].[Cl:1][C:2]1[CH:3]=[C:4]([N:9]([CH2:50][C:51]([F:54])([F:53])[F:52])[C:10](=[O:31])[CH2:11][N:12]2[CH:16]=[C:15]([C:17]3[CH:22]=[CH:21][C:20]([N:23]4[CH:27]=[C:26]([CH3:28])[N:25]=[CH:24]4)=[C:19]([O:29][CH3:30])[CH:18]=3)[N:14]=[N:13]2)[CH:5]=[CH:6][C:7]=1[F:8]N-(3-chloro-4-fluorophenyl)-2-{-4-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]-1H-1,2,3-triazol-1-yl}acetamide (50 mg, 0.113 mmol) and KHMDS (27.1 mg, 0.136 mmol) were added to a 25-mL flask under nitrogen and DMF (3 ml) was added. Trifluoroethyl triflate (0.023 ml, 0.159 mmol) was added and the suspension stirred at room temperature for 16 h. The residue was purified by preparative HPLC Reverse phase (C-18), eluting with Acetonitrile/Water+0.1% TFA, to give the product (25 mg) as a yellow solid.
Wird geladen…