C(OC([NH:8][C@H:9]([C:14]([O:16][CH2:17][CH2:18][O:19][C:20]1[CH:25]=[CH:24][C:23]([C:26]2[C:31]([C:32]#[N:33])=[C:30]([N:34]3[CH2:38][CH2:37][CH2:36][CH2:35]3)[N:29]=[C:28]([S:39][CH2:40][C:41]3[N:42]=[C:43]([C:46]4[CH:51]=[CH:50][C:49]([Cl:52])=[CH:48][CH:47]=4)[S:44][CH:45]=3)[C:27]=2[C:53]#[N:54])=[CH:22][CH:21]=1)=[O:15])[CH2:10][CH:11]([CH3:13])[CH3:12])=O)(C)(C)C.[F:55][C:56]([F:61])([F:60])[C:57]([OH:59])=[O:58]>ClCCl>[F:55][C:56]([F:61])([F:60])[C:57]([OH:59])=[O:58].[NH2:8][C@H:9]([C:14]([O:16][CH2:17][CH2:18][O:19][C:20]1[CH:21]=[CH:22][C:23]([C:26]2[C:31]([C:32]#[N:33])=[C:30]([N:34]3[CH2:38][CH2:37][CH2:36][CH2:35]3)[N:29]=[C:28]([S:39][CH2:40][C:41]3[N:42]=[C:43]([C:46]4[CH:51]=[CH:50][C:49]([Cl:52])=[CH:48][CH:47]=4)[S:44][CH:45]=3)[C:27]=2[C:53]#[N:54])=[CH:24][CH:25]=1)=[O:15])[CH2:10][CH:11]([CH3:12])[CH3:13]1.37 g (1.74 mmol) of 2-{4-(2-({(2-(4-chlorophenyl)-1,3-thiazol-4-yl)methyl}sulfanyl)-3,5-dicyano-6-(pyrrolidin-1-yl)pyridin-4-yl)phenoxy}ethyl N-(tert-butoxycarbonyl)-L-leucinate were initially charged in 15 ml of dichloromethane, and 15.00 ml (194.70 mmol) of trifluoroacetic acid were added. The mixture was stirred at room temperature for 1 h. After removal of the solvent under reduced pressure, the residue was dissolved in 5.00 ml of dichloromethane and 10.00 ml of diethyl ether were added. The residue formed was filtered off with suction. Drying gave 1.09 g (76.1% of theory) of the desired target compound.
Wird geladen…