[C:1]([O:5][C:6]([NH:8][CH2:9][C:10]1[C:11]([CH2:35][CH:36]([CH3:38])[CH3:37])=[N:12][C:13]2[C:18]([C:19]=1[C:20]1[CH:25]=[CH:24][C:23]([CH3:26])=[CH:22][CH:21]=1)=[CH:17][C:16]([C:27]1[S:28][CH:29]=[C:30]([C:32]([OH:34])=[O:33])[N:31]=1)=[CH:15][CH:14]=2)=[O:7])([CH3:4])([CH3:3])[CH3:2].[CH:39](O)([CH3:41])[CH3:40].C1CCN(C(/N=N/C(N2CCCCC2)=O)=O)CC1>O1CCCC1>[C:1]([O:5][C:6]([NH:8][CH2:9][C:10]1[C:11]([CH2:35][CH:36]([CH3:38])[CH3:37])=[N:12][C:13]2[C:18]([C:19]=1[C:20]1[CH:25]=[CH:24][C:23]([CH3:26])=[CH:22][CH:21]=1)=[CH:17][C:16]([C:27]1[S:28][CH:29]=[C:30]([C:32]([O:34][CH:39]([CH3:41])[CH3:40])=[O:33])[N:31]=1)=[CH:15][CH:14]=2)=[O:7])([CH3:3])([CH3:2])[CH3:4]To a mixture of 2-[3-{[(tert-butoxycarbonyl)amino]methyl}-2-isobutyl-4-(4-methylphenyl)quinolin-6-yl]-1,3-thiazole-4-carboxylic acid (0.26 g, 0.5 mmol), n-tributylphosphine (0.25 ml, 1.0 mmol), isopropanol (0.5 ml) and tetrahydrofuran (10 ml) was added 1,1-(azodicarbonyl)dipiperidine (0.25 g, 1.0 mmol), and the mixture was stirred at room temperature for 2 hrs. Precipitated crystals were removed and the solvent was evaporated. The residue was purified by silica gel column chromatography to give isopropyl 2-[3-{[(tert-butoxycarbonyl)amino]methyl}-2-isobutyl-4-(4-methylphenyl)quinolin-6-yl]-1,3-thiazole-4-carboxylate (0.20 g, yield 71%) as white crystals.
Wird geladen…