3-Methanesulfonyl-5-(trifluoromethyl)benzoic acid → N-(4-(2-(benzyloxy)phenyl)-6-methylpyridin-3-yl)-N-methyl-3-(methylsulfonyl)-5-(trifluoromethyl)benzamide
반응식
[CH2:1]([O:8][C:9]1[CH:14]=[CH:13][CH:12]=[CH:11][C:10]=1[C:15]1[CH:20]=[C:19]([CH3:21])[N:18]=[CH:17][C:16]=1[NH:22][CH3:23])[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.[CH3:24][S:25]([C:28]1[CH:29]=[C:30]([CH:34]=[C:35]([C:37]([F:40])([F:39])[F:38])[CH:36]=1)[C:31]([OH:33])=O)(=[O:27])=[O:26]>>[CH2:1]([O:8][C:9]1[CH:14]=[CH:13][CH:12]=[CH:11][C:10]=1[C:15]1[CH:20]=[C:19]([CH3:21])[N:18]=[CH:17][C:16]=1[N:22]([CH3:23])[C:31](=[O:33])[C:30]1[CH:34]=[C:35]([C:37]([F:40])([F:39])[F:38])[CH:36]=[C:28]([S:25]([CH3:24])(=[O:26])=[O:27])[CH:29]=1)[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1참가 물질
3
실험 절차
The title compound was prepared in analogy to example 90, from 4-(2-(benzyloxy)phenyl)-N,6-dimethylpyridin-3-amine and 3-(methylsulfonyl)-5-(trifluoromethyl)benzoic acid (1.49 g, 5.55 mmol, example 114, intermediate a) after a reaction time of 3.5 days at room temperature. The compound was purified by silica gel chromatography on a 50 g column using an MPLC system (CombiFlash Companion, Isco Inc.) eluting with a gradient of n-heptane:EtOAc (100:0 to 10:90). Off-white solid (53%). MS (ESI): m/z=555.156 [M+H]+.