反応式
Br[C:2]1[S:6][C:5]([NH:7][C:8](=[O:17])[C:9]2[C:14]([F:15])=[CH:13][CH:12]=[CH:11][C:10]=2[F:16])=[N:4][C:3]=1[CH3:18].[CH3:19][C:20]1[CH:25]=[CH:24][C:23]([C:26]2[O:27][CH:28]=[CH:29][N:30]=2)=[CH:22][C:21]=1B1OC(C)(C)C(C)(C)O1.C([O-])(O)=O.[Na+].C1(P(C2C=CC=CC=2)CCCCP(C2C=CC=CC=2)C2C=CC=CC=2)C=CC=CC=1>C1(C)C=CC=CC=1.C1C=CC(C#N)=CC=1.C1C=CC(C#N)=CC=1.Cl[Pd]Cl>[F:16][C:10]1[CH:11]=[CH:12][CH:13]=[C:14]([F:15])[C:9]=1[C:8]([NH:7][C:5]1[S:6][C:2]([C:21]2[CH:22]=[C:23]([C:26]3[O:27][CH:28]=[CH:29][N:30]=3)[CH:24]=[CH:25][C:20]=2[CH3:19])=[C:3]([CH3:18])[N:4]=1)=[O:17]参加物
7
反応物 4
生成物 1
試薬・触媒・溶媒 2
反応条件
- 温度
- 170 °C
実験手順
N-(5-bromo-4-methylthiazol-2-yl)-2,6-difluorobenzamide (60 mg), 2-(4-methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)oxazole (70 mg), 2 M NaHCO3 solution (0.5 mL), dichlorobis(benzonitrile)palladium (5 mg) and 1,4-Bis(diphenyl-phosphino)butane (10 mg) were mixed together in 2 mL of toluene in a sealed tube. The resulting suspension was stirred in microwave oven at 170° C. for 1 hour. After the reaction, the mixture was extracted with Et2O. The organic phases were removed under reduced pressure and the residue was chromatographed to give the title compound as a white solid. Yield 27%.
後処理
- customAfter the reaction
- extractionthe mixture was extracted with Et2O
- customThe organic phases were removed under reduced pressure
- customthe residue was chromatographed
出典と根拠
- ORDレコード
- ord-b2d4eb74dbd045a182234104a99c606f
- 出典データセット
- uspto-grants-2013_06
- 特許番号
- US08455658B2
関連ノート
読み込み中…