CS(O[CH:6]([C:19]1[CH:20]=[N:21][C:22]([NH:51][C:52]2[CH:53]=[N:54][C:55]([O:58][CH3:59])=[CH:56][CH:57]=2)=[C:23]([C:25]2[N:30]=[C:29]([N:31]([CH2:41][C:42]3[CH:47]=[CH:46][C:45]([O:48][CH3:49])=[CH:44][CH:43]=3)[CH2:32][C:33]3[CH:38]=[CH:37][C:36]([O:39][CH3:40])=[CH:35][CH:34]=3)[N:28]=[C:27]([CH3:50])[N:26]=2)[CH:24]=1)[C:7]1[CH:12]=[CH:11][C:10]([S:13](=[O:18])(=[O:17])[N:14]([CH3:16])[CH3:15])=[CH:9][CH:8]=1)(=O)=O.[NH3:60]>C(Cl)Cl.O1CCOCC1>[NH2:60][CH:6]([C:19]1[CH:20]=[N:21][C:22]([NH:51][C:52]2[CH:53]=[N:54][C:55]([O:58][CH3:59])=[CH:56][CH:57]=2)=[C:23]([C:25]2[N:30]=[C:29]([N:31]([CH2:32][C:33]3[CH:34]=[CH:35][C:36]([O:39][CH3:40])=[CH:37][CH:38]=3)[CH2:41][C:42]3[CH:47]=[CH:46][C:45]([O:48][CH3:49])=[CH:44][CH:43]=3)[N:28]=[C:27]([CH3:50])[N:26]=2)[CH:24]=1)[C:7]1[CH:12]=[CH:11][C:10]([S:13]([N:14]([CH3:15])[CH3:16])(=[O:18])=[O:17])=[CH:9][CH:8]=1A solution of (5-(4-(bis(4-methoxybenzyl)amino)-6-methyl-1,3,5-triazin-2-yl)-6-(6-methoxypyridin-3-ylamino)pyridin-3-yl)(4-(N,N-dimethylsulfamoyl)phenyl)methyl methanesulfonate (14.22 mg, 0.017 mmol) in DCM (0.1 mL) was treated with 0.5 M NH3 in dioxane (2 mL). The mixture was allowed to stand overnight, after which time partial conversion to the amine was observed by LCMS. The mixture was then sealed and heated and 80° C. for 2 h, after which time the starting material was consumed. The mixture was concentrated and taken on directly to the next step.
Wird geladen…