[CH3:1][O:2][C:3]1[CH:4]=[C:5]([NH:11][C:12]([C:14]2[CH:28]=[CH:27][C:17]3[N:18]=[C:19]([N:21]4[CH2:26][CH2:25][NH:24][CH2:23][CH2:22]4)[S:20][C:16]=3[CH:15]=2)=[O:13])[CH:6]=[CH:7][C:8]=1[O:9][CH3:10].[CH3:29][C:30]([O:33][C:34]([NH:36][C@H:37]([C:44](O)=[O:45])[CH2:38][C:39]1[S:43][CH:42]=[CH:41][CH:40]=1)=[O:35])([CH3:32])[CH3:31].C(N(C(C)C)CC)(C)C.CN(C(ON1N=NC2C=CC=CC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F>CN(C=O)C.C(OCC)(=O)C>[CH3:1][O:2][C:3]1[CH:4]=[C:5]([NH:11][C:12]([C:14]2[CH:28]=[CH:27][C:17]3[N:18]=[C:19]([N:21]4[CH2:26][CH2:25][N:24]([C:44](=[O:45])[C@@H:37]([NH:36][C:34](=[O:35])[O:33][C:30]([CH3:29])([CH3:31])[CH3:32])[CH2:38][C:39]5[S:43][CH:42]=[CH:41][CH:40]=5)[CH2:23][CH2:22]4)[S:20][C:16]=3[CH:15]=2)=[O:13])[CH:6]=[CH:7][C:8]=1[O:9][CH3:10]N-(3,4-dimethoxyphenyl)-2-(piperazin-1-yl)benzo[d]thiazole-6-carboxamide (1.00 g, 2.51 mmol), Boc-L-2-thienylalanine (0.68 g, 2.551 mmol), diisopropylethylamine (1.75 ml, 10.04 mmol) and HBTU (1.24 g, 3.26 mmol) were dissolved in DMF (71 ml) and stirred overnight. The resulting mixture was diluted with ethyl acetate (154 ml), washed with 1N HCl (3×77 ml), washed with brine (77 ml), dried (MgSO4) and concentrated in vacuo. The resulting residue was chromatographed, eluting with dichloromethane/methanol (97:3) to yield (S)-tert-butyl 1-(4-(6-(3,4-dimethoxyphenylcarbamoyl)benzo[d]thiazol-2-yl)piperazin-1-yl)-1-oxo-3-(thiophen-2-yl)propan-2-ylcarbamate.
読み込み中…