[Cl:1][C:2]1[CH:7]=[CH:6][CH:5]=[C:4]([Cl:8])[C:3]=1[CH2:9][S:10]([C:13]1[CH:14]=[C:15]2[C:19](=[CH:20][CH:21]=1)[NH:18][C:17](=[O:22])/[C:16]/2=[CH:23]\[C:24]1[NH:28][C:27]([CH3:29])=[C:26]([CH2:30][C:31]([OH:33])=O)[C:25]=1[CH3:34])(=[O:12])=[O:11].[F:35][C:36]([F:43])([F:42])[CH2:37][NH:38][CH2:39][CH2:40][NH2:41].C1C=CC2N(O)N=NC=2C=1.CCN=C=NCCCN(C)C>CN(C=O)C>[Cl:1][C:2]1[CH:7]=[CH:6][CH:5]=[C:4]([Cl:8])[C:3]=1[CH2:9][S:10]([C:13]1[CH:14]=[C:15]2[C:19](=[CH:20][CH:21]=1)[NH:18][C:17](=[O:22])/[C:16]/2=[CH:23]\[C:24]1[NH:28][C:27]([CH3:29])=[C:26]([CH2:30][C:31]([NH:41][CH2:40][CH2:39][NH:38][CH2:37][C:36]([F:43])([F:42])[F:35])=[O:33])[C:25]=1[CH3:34])(=[O:11])=[O:12]A mixture of {5-[5-(2,6-dichloro-phenylmethanesulfonyl)-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrol-3-yl}-acetic acid (267 mg, 0.51 mmol), N-(2,2,2-trifluoro-ethyl)-ethane-1,2-diamine (123 mg, 0.86 mmol), HOBt (104 mg, 0.77 mmol), EDAC (154 mg, 0.81 mmol) and TEA (0.14 mL, 1 mmol) in DMF (3 mL) was stirred At rt for 48 hours. The reaction was concentrated, diluted with sat. sodium bicarbonate and extracted with DCM. The organic layer was washed with brine, dried and purified on a silica gel column to give 237 mg (72%) of the titled compound.
Wird geladen…