Triethylamine → 4-Chloro-7-(1-methylindol-2-yl)isoindolinone

HRID 21103ノート

反応式

HRID 21103 の反応式
[Cl:1][C:2]1[CH:10]=[CH:9][C:8](I)=[C:7]2[C:3]=1[CH2:4][NH:5][C:6]2=[O:12].[CH2:13]([N:15]([CH2:18][CH3:19])[CH2:16][CH3:17])C>C(#N)C.C([O-])(=O)C.[Pd+2].C([O-])(=O)C>[Cl:1][C:2]1[CH:10]=[CH:9][C:8]([C:16]2[N:15]([CH3:13])[C:18]3[C:19]([CH:17]=2)=[CH:4][CH:3]=[CH:2][CH:10]=3)=[C:7]2[C:3]=1[CH2:4][NH:5][C:6]2=[O:12]

参加物

5

反応物 2

HCID 8471TriethylamineHCID 684927354-Chloro-7-iodoisoindolinone

生成物 1

HCID 684922684-Chloro-7-(1-methylindol-2-yl)isoindolinone収率 164.2%

試薬・触媒・溶媒 2

HCID 167845palladium(II) acetate触媒HCID 6342Acetonitrile溶媒

実験手順

In a similar manner to Step 2 of Example 1, 4-chloro-7-iodoisoindolinone (84.0 mg, 0.286 mmol) was dissolved in acetonitrile (3 mL), and the solution was treated with Compound BK (100 mg, 0.571 mmol), palladium acetate (5.2 mg, 0.023 mmol) and triethylamine (0.400 mL, 2.87 mmol), followed by purification by flash column chromatography (hexane/ethyl acetate=7/3, 3/2, 1/1) to obtain Compound 156 (69.7 mg, yield 82%).

後処理

  1. customfollowed by purification by flash column chromatography (hexane/ethyl acetate=7/3, 3/2, 1/1)

出典と根拠

ORDレコード
ord-62ee8151a279485585f17aa92ecaaf07
出典データセット
uspto-grants-2010_06
特許番号
US07745641B2

反応ノート

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