反応式
FC(F)(F)S(O[C:7]1[CH:15]=[CH:14][C:13]([C:16]2[N:17]([C:32]([O:34][C:35]([CH3:38])([CH3:37])[CH3:36])=[O:33])[C:18]3[C:23]([CH:24]=2)=[CH:22][C:21]([CH2:25][N:26]2[CH2:31][CH2:30][CH2:29][CH2:28][CH2:27]2)=[CH:20][CH:19]=3)=[C:12]2[C:8]=1[CH2:9][NH:10][C:11]2=[O:39])(=O)=O.[CH2:42]1[O:50][C:49]2[CH:48]=[CH:47][C:46](B(O)O)=[CH:45][C:44]=2[O:43]1.C(=O)([O-])[O-].[K+].[K+].O>C(COC)OC.C(Cl)(Cl)Cl.CO.C(#N)C>[O:43]1[C:44]2[CH:45]=[CH:46][C:47]([C:7]3[CH:15]=[CH:14][C:13]([C:16]4[N:17]([C:32]([O:34][C:35]([CH3:36])([CH3:38])[CH3:37])=[O:33])[C:18]5[C:23]([CH:24]=4)=[CH:22][C:21]([CH2:25][N:26]4[CH2:31][CH2:30][CH2:29][CH2:28][CH2:27]4)=[CH:20][CH:19]=5)=[C:12]4[C:8]=3[CH2:9][NH:10][C:11]4=[O:39])=[CH:48][C:49]=2[O:50][CH2:42]1参加物
7
反応物 4
生成物 1
試薬・触媒・溶媒 2
実験手順
In a similar manner to Step 1 of Example 152, 4-trifluoromethanesulfonyloxy-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone (50.0 mg, 0.0842 mmol) was dissolved in dimethoxyethane (4 mL), and the solution was treated with 3,4-methylenedioxybenzeneboronic acid (70.0 mg, 0.421 mmol). [bis(diphenylphosphino)ferrocene]dichloropalladium (13.7 mg, 0.0168 mmol), potassium carbonate (116 mg, 0.842 mmol) and water (0.060 mL), followed by purification by preparative thin-layer chromatography (chloroform/methanol/acetonitrile=8/0.5/0.5 to 0.4/0.5/0.5) to obtain 4-(benzo[1,3]dioxol-5-yl)-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone (22.2 mg, yield 47%).
出典と根拠
- ORDレコード
- ord-c5f29237513f4f30b616272ed3d873f2
- 出典データセット
- uspto-grants-2010_06
- 特許番号
- US07745641B2
関連ノート
読み込み中…