2-(Tri-n-butylstannyl)thiophene → 7-Amino-4-(thiophen-2-yl)isoindolinone

HRID 21095

반응식

HRID 21095 반응식
[NH2:1][C:2]1[CH:3]=[CH:4][C:5](Br)=[C:6]2[C:10]=1[C:9](=[O:11])[NH:8][CH2:7]2.C([Sn](CCCC)(CCCC)[C:18]1[S:19][CH:20]=[CH:21][CH:22]=1)CCC>C1COCC1.Cl[Pd](Cl)([P](C1C=CC=CC=1)(C1C=CC=CC=1)C1C=CC=CC=1)[P](C1C=CC=CC=1)(C1C=CC=CC=1)C1C=CC=CC=1>[NH2:1][C:2]1[CH:3]=[CH:4][C:5]([C:18]2[S:19][CH:20]=[CH:21][CH:22]=2)=[C:6]2[C:10]=1[C:9](=[O:11])[NH:8][CH2:7]2

참가 물질

5

반응물 2

HCID 27793732-(Tri-n-butylstannyl)thiopheneHCID 197019327-Amino-4-bromo-2,3-dihydroisoindol-1-one

생성물 1

HCID 684924787-Amino-4-(thiophen-2-yl)isoindolinone수율 54%

시약·촉매·용매 2

HCID 178418476HCID 178418476, 화합물촉매HCID 8028Tetrahydrofuran용매

실험 절차

In a similar manner to Step 1 of Example 10, 7-amino-4-bromoisoindolinone (404 mg, 1.78 mmol) was dissolved in THF (20 mL), and the solution was treated with 2-(tributylstannyl)thiophene (1.13 mL, 3.56 mmol) and bis(triphenylphosphine)dichloropalladium (100 mg, 0.142 mmol), followed by purification by preparative thin-layer chromatography (chloroform/methanol=12/1) to obtain 7-amino-4-(thiophen-2-yl)isoindolinone (220 mg, yield 54%).

후처리

  1. customfollowed by purification by preparative thin-layer chromatography (chloroform/methanol=12/1)

출처 및 근거

ORD 기록
ord-4bfbc436ac3f44c8b9a69949eb1f4ac1
출처 데이터셋
uspto-grants-2010_06
특허 번호
US07745641B2

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