[C:1]([O:5][C:6]([N:8]1[CH2:13][CH2:12][CH:11]([O:14][C:15]2[CH:20]=[CH:19][C:18]([NH:21][CH2:22][CH:23]=[CH:24][C:25]3[C:30]([O:31][CH2:32][C:33]4[CH:38]=[CH:37][C:36]([O:39][CH3:40])=[CH:35][CH:34]=4)=[CH:29][CH:28]=[C:27]([C:41]#[N:42])[CH:26]=3)=[CH:17][C:16]=2[C:43]([F:46])([F:45])[F:44])[CH2:10][CH2:9]1)=[O:7])([CH3:4])([CH3:3])[CH3:2].Cl[C:48](=[O:56])[CH2:49][CH2:50][C:51]([O:53][CH2:54][CH3:55])=[O:52].N1C=CC=CC=1>C(Cl)Cl>[C:1]([O:5][C:6]([N:8]1[CH2:9][CH2:10][CH:11]([O:14][C:15]2[CH:20]=[CH:19][C:18]([N:21]([C:48]([CH2:49][CH2:50][C:51]([O:53][CH2:54][CH3:55])=[O:52])=[O:56])[CH2:22][CH:23]=[CH:24][C:25]3[C:30]([O:31][CH2:32][C:33]4[CH:38]=[CH:37][C:36]([O:39][CH3:40])=[CH:35][CH:34]=4)=[CH:29][CH:28]=[C:27]([C:41]#[N:42])[CH:26]=3)=[CH:17][C:16]=2[C:43]([F:46])([F:44])[F:45])[CH2:12][CH2:13]1)=[O:7])([CH3:4])([CH3:2])[CH3:3]To 4-(N′-(t-butoxycarbonyl)piperidin-4-yl)oxy-3-trifluoromethyl-N-(3-(6-((4-methoxybenzyl)oxy)-3-cyanophenyl)prop-2-en-1-yl)benzenamine (1.39 g) in 20 mL of CH2Cl2 was added ethyl 4-chloro-4-oxobutyrate (0.43 g) and pyridine (1 mL) at 0° C. The resulting solution was allowed to warm to ambient temperature for 30 minutes and then diluted with 100 mL CH2Cl2. The organic layer was washed with saturated copper sulfate, dried and concentrated to afford 4-(N′-(t-butoxycarbonyl)piperidin-4-yl)oxy-3-trifluoromethyl-N-(2-(ethoxycarbonyl)ethylcarbonyl)-N-(3-(6-((4-methoxybenzyl)oxy)-3-cyanophenyi)prop-2-en-1-yl)benzenamine as a blue solid.
読み込み中…