[C:1]([O:5][C:6]([C@@H:8]([NH:23][S:24]([C:27]1[CH:32]=[CH:31][C:30]([C:33]([F:36])([F:35])[F:34])=[CH:29][CH:28]=1)(=[O:26])=[O:25])[CH2:9][C:10]1[CH:22]=[CH:21][C:13]([O:14][CH2:15][CH2:16][CH2:17][C:18](O)=[O:19])=[CH:12][CH:11]=1)=[O:7])([CH3:4])([CH3:3])[CH3:2].C([N:40](C(C)C)CC)(C)C.CN(C(O[N:54]1N=NC2[CH:57]=[CH:58][CH:59]=[N:60][C:55]1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F>O1CCCC1.N1CCCN=C1N>[C:1]([O:5][C:6](=[O:7])[C@@H:8]([NH:23][S:24]([C:27]1[CH:28]=[CH:29][C:30]([C:33]([F:34])([F:35])[F:36])=[CH:31][CH:32]=1)(=[O:25])=[O:26])[CH2:9][C:10]1[CH:11]=[CH:12][C:13]([O:14][CH2:15][CH2:16][CH2:17][C:18](=[O:19])[NH:40][C:55]2[NH:54][CH2:57][CH2:58][CH2:59][N:60]=2)=[CH:21][CH:22]=1)([CH3:2])([CH3:3])[CH3:4]56 mg of 4-{4-[(2S)-2-tert-butoxycarbonyl-2-(4-trifluoromethylbenzenesulfonylamino)-ethyl]-phenoxy}-butyric acid were dissolved in tetrahydrofuran and 12.5 mg of 1,4,5,6-tetrahydropyrimidin-2-ylamine, 68 mg of diisopropylethylamine and 44 mg of HATU were added. The reaction mixture was stirred overnight, and the solvent was removed in vacuo. The residue was dissolved in dichloromethane and washed with saturated aqueous sodium bicarbonate solution and saturated aqueous sodium chloride solution. The organic phase was dried with sodium sulfate, filtered and the solvent was removed in vacuo. The residue was chromatographed on reversed-phase (C-18) silica gel eluting with a gradient of 10-90% acetonitrile in water. Yield 37.3 mg. MS (FAB+): m/e=613.3 (M+H)+.
Wird geladen…