反応式
Cl[C:2]1[CH:11]=[CH:10][C:9]2[C:4](=[CH:5][CH:6]=[CH:7][C:8]=2[NH:12][S:13]([C:16]2[CH:21]=[C:20]([F:22])[CH:19]=[C:18]([F:23])[CH:17]=2)(=[O:15])=[O:14])[N:3]=1.[CH3:24][C:25]1[O:26][C:27]2[C:33]([NH2:34])=[CH:32][CH:31]=[CH:30][C:28]=2[CH:29]=1>O1CCOCC1>[F:23][C:18]1[CH:17]=[C:16]([S:13]([NH:12][C:8]2[CH:7]=[CH:6][CH:5]=[C:4]3[C:9]=2[CH:10]=[CH:11][C:2]([NH:34][C:33]2[C:27]4[O:26][C:25]([CH3:24])=[CH:29][C:28]=4[CH:30]=[CH:31][CH:32]=2)=[N:3]3)(=[O:15])=[O:14])[CH:21]=[C:20]([F:22])[CH:19]=1参加物
4
反応条件
- 温度
- 100 °C
実験手順
N-(2-Chloro-quinolin-5-yl)-3,5-difluoro-benzenesulfonamide (150 mg, 0.423 mmol) was dissolved in 3 mL dioxane. Argon was bubbled through the solution for 2 minutes to remove oxygen. (2-Methyl-1-benzofuran-7-yl)amine (245 mg, 1.33 mmol), sodium tert.-butylate (230 mg, 2.40 mmol), 1,1′-bis(diphenylphosphin)ferrocen (36 mg, 0.06 mmol) and 1,1′-bis(diphenylphosphin)ferrocen-palladium(II)chloride (17 mg, 0.02 mmol) were added. The reaction mixture was stirred in a sealed tube at 100° C. for 16 h. The solvent was evaporated and the residue purified by flash chromatography on silica gel (heptane/ethyl acetate 100:0->60:40 gradient). The title compound was obtained as a light brown solid (164 mg, 83%), MS: m/e=466.0 (M+H+).
後処理
- customArgon was bubbled through the solution for 2 minutes
- customto remove oxygen
- customThe solvent was evaporated
- customthe residue purified by flash chromatography on silica gel (heptane/ethyl acetate 100:0->60:40 gradient)
出典と根拠
- ORDレコード
- ord-123b2c376a72419bbe4f04164744dcf8
- 出典データセット
- uspto-grants-2010_11
- 特許番号
- US07825253B2
関連ノート
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