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

HRID 21103노트

반응식

HRID 21103 반응식
[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]

참가 물질

5

반응물 2

HCID 8471TriethylamineHCID 684927354-Chloro-7-iodoisoindolinone

생성물 1

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

시약·촉매·용매 2

HCID 167845palladium(II) acetate촉매HCID 6342Acetonitrile용매

실험 절차

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%).

후처리

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

출처 및 근거

ORD 기록
ord-62ee8151a279485585f17aa92ecaaf07
출처 데이터셋
uspto-grants-2010_06
특허 번호
US07745641B2

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