참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Isopropanol | HCID 3776 | — |
| 반응물 | Triethylamine | HCID 8471 | — |
| 반응물 | Potassium vinyltrifluoroborate | HCID 23679353 | — |
| 반응물 | 3-iodo-1-((6-methylpyridin-2-yl)methyl)-4-nitro-1H-indazole | HCID 67259762 | — |
| 용매 | Tetrahydrofuran | HCID 8028 | — |
| 생성물 | 1-((6-methylpyridin-2-yl)methyl)-4-nitro-3-vinyl-1H-indazole | HCID 67259703 | 87.4% |
반응 단계
To a reaction vial was added 3-iodo-1-((6-methylpyridin-2-yl)methyl)-4-nitro-1H-indazole (216 mg, 0.548 mmol) and potassium trifluoro(vinyl)borate (156 mg, 1.64 mmol). Isopropanol (2 mL) and tetrahydrofuran (0.5 mL) were added. Argon was bubbled through the mixture for 20 minutes. Triethylamine (229 μL, 1.64 mmol) and 1,1′-bis(diphenylphosphino)ferrocene-palladium(II)dichloride dichloromethane complex (44.8 mg, 0.0548 mmol) were added. The vial was sealed and the mixture was heated at 90-100° C. for 3 hours. The mixture was allowed to cool and filtered through glass fiber filter paper, washing with ethyl acetate. The solution was concentrated under reduced pressure. The residue was dissolved in chloroform (30 mL) and washed with water (10 mL). The solution was dried over magnesium sulfate, filtered and concentrated under reduced pressure to give 1-((6-methylpyridin-2-yl)methyl)-4-nitro-3-vinyl-1H-indazole as an oil (141 mg).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US08841455B2 |
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| 출처 데이터셋 | uspto-grants-2014_09 |
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| ORD ID | ord-d095b51903c94877b397a4f239969812 |
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| 출처 메모 | uspto-grants-2014_09 |
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