6-[(4-acetyl-2,6-dichlorophenyl)amino]pyrido[4,3-c]-1,6-naphthyridin-10(9H)-one → 6-{[2,6-Dichloro-4-(1-hydroxy-1-methylethyl)phenyl]amino}pyrido[4,3-c]-1,6-naphthyridin-10(9H)-one
反応式
[C:1]([C:4]1[CH:9]=[C:8]([Cl:10])[C:7]([NH:11][C:12]2[C:21]3[CH:22]=[CH:23][NH:24][C:25](=[O:26])[C:20]=3[C:19]3[C:14](=[CH:15][CH:16]=[N:17][CH:18]=3)[N:13]=2)=[C:6]([Cl:27])[CH:5]=1)(=[O:3])[CH3:2].[CH3:28][Mg]Br>C1COCC1>[Cl:27][C:6]1[CH:5]=[C:4]([C:1]([OH:3])([CH3:28])[CH3:2])[CH:9]=[C:8]([Cl:10])[C:7]=1[NH:11][C:12]1[C:21]2[CH:22]=[CH:23][NH:24][C:25](=[O:26])[C:20]=2[C:19]2[C:14](=[CH:15][CH:16]=[N:17][CH:18]=2)[N:13]=1参加物
4
実験手順
To a solution of 6-[(4-acetyl-2,6-dichlorophenyl)amino]pyrido[4,3-c]-1,6-naphthyridin-10(9H)-one (Examples 144 and 145, Step 3) (1.3 g, 3.26 mmol) in THF (30 mL) at 0° C. under nitrogen atmosphere was added methyl magnesium bromide (11.6 mL, 1.4 M in THF/toluene) and the reaction mixture stirred for 30 min. The solution was quenched with 1 N citric acid, diluted with 1:1 THF/EtOAc, and neutralized with saturated NaHCO3. The organic layer was concentrated, triturated with diethyl ether, and filtered to afford the desired product as a yellow powder.