[CH2:1]([C:3]1[C:11]2[C:6](=[CH:7][CH:8]=[CH:9][C:10]=2[NH:12][C:13]([C:15]2[N:19]3[CH:20]=[CH:21][CH:22]=[CH:23][C:18]3=[N:17][CH:16]=2)=[O:14])[N:5]([CH2:24][C:25]2[CH:30]=[CH:29][CH:28]=[C:27]([OH:31])[N:26]=2)[N:4]=1)[CH3:2].CS(O[CH2:37][CH:38]1[CH2:42][O:41][C:40]([CH3:44])([CH3:43])[O:39]1)(=O)=O.C([O-])([O-])=O.[Cs+].[Cs+]>CC(N(C)C)=O>[CH3:43][C:40]1([CH3:44])[O:39][CH:38]([CH2:37][O:31][C:27]2[N:26]=[C:25]([CH2:24][N:5]3[C:6]4[C:11](=[C:10]([NH:12][C:13]([C:15]5[N:19]6[CH:20]=[CH:21][CH:22]=[CH:23][C:18]6=[N:17][CH:16]=5)=[O:14])[CH:9]=[CH:8][CH:7]=4)[C:3]([CH2:1][CH3:2])=[N:4]3)[CH:30]=[CH:29][CH:28]=2)[CH2:42][O:41]1To N-(3-ethyl-1-((6-hydroxypyridin-2-yl)methyl)-1H-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide (17, Step A) (16 mg, 0.039 mmol) in DMA (2 mL) was added (2,2-dimethyl-1,3-dioxolan-4-yl)methyl methanesulfonate (8.2 mg, 0.039 mmol) and Cs2CO3 (25 mg, 0.078 mmol). The reaction vial was sealed and the mixture was heated at 90° C. for 6 hours. The DMA was removed under reduced pressure. The residue was diluted with EtOAc (20 mL). The organic solution was washed with saturated NaHCO3 aqueous solution and brine, and then concentrated under reduced pressure. Silica gel chromatography (DCM/MeOH 10:0.5) gave the product (12 mg).
Wird geladen…