[C:1]([O:5][C:6](=[O:17])[NH:7][C:8]1[S:9][C:10]([CH:13]([OH:16])[CH2:14][NH2:15])=[CH:11][N:12]=1)([CH3:4])([CH3:3])[CH3:2].Cl[C:19]1[C:20]2[S:27][CH:26]=[CH:25][C:21]=2[N:22]=[CH:23][N:24]=1.CCN(C(C)C)C(C)C>CC(N(C)C)=O>[C:1]([O:5][C:6](=[O:17])[NH:7][C:8]1[S:9][C:10]([CH:13]([OH:16])[CH2:14][NH:15][C:19]2[C:20]3[S:27][CH:26]=[CH:25][C:21]=3[N:22]=[CH:23][N:24]=2)=[CH:11][N:12]=1)([CH3:4])([CH3:2])[CH3:3]Compound 62.4 (0.16 mmol), 4-chloro-thieno[3,2-d]pyrimidine (0.16 mmol.) and DIEA (0.28 mmol) is heated in DMA at 90° C. for 5 hours. The reaction mixture is cooled, concentrated and purified by preparative TLC (10% MeOH in EtOAc) to afford {5-[1-hydroxy-2-(thieno[3,2-d]pyrimidin-4-ylamino)-ethyl]-thiazol-2-yl}-carbamic acid tert-butyl ester (compound 62.5).
Wird geladen…