Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 60094생성일: 2026년 10월 25일
Potassium Carbonate → 2-fluoro-N-(2-fluoro-3-[5-(2-methoxy-pyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-benzenesulfonamide
https://huagongshe.com/reaction/60094
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Potassium Carbonate | HCID 11430 | — |
| 반응물 | 2-Methoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidine | HCID 53440592 | — |
| 반응물 | HCID 58368734 | HCID 58368734 | — |
| 촉매 | Tetrakis(triphenylphosphine)palladium | HCID 11979704 | — |
| 용매 | Acetonitrile | HCID 6342 | — |
| 생성물 | 2-fluoro-N-(2-fluoro-3-[5-(2-methoxy-pyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-benzenesulfonamide | HCID 58368758 | 25.5% |
반응 단계
In a microwave vial, N-[3-(5-bromo-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2-fluoro-phenyl]-2-fluoro-benzenesulfonamide (21, 100 mg, 0.203 mmol), 2-methoxy-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-pyrimidine (22, 72 mg, 0.305 mmol) and tetrakis-(triphenylphosphine) palladium(0) (10 mg) are combined with potassium carbonate (0.609 mL, 1M aqueous, 0.609 mmol) and 0.6 mL of acetonitrile. The reaction mixture is heated in a microwave at 160° C. for 15 minutes. The mixture is filtered through celite, and the celite is washed with water and ethyl acetate. The aqueous layer is separated from the filtrate and extracted with ethyl acetate. The organic portions are combined and washed with brine, then dried over sodium sulfate, filtered and the filtrate concentrated under vacuum. The resulting material is purified by silica gel column chromatography, eluting with methanol and dichloromethane. Appropriate fractions are combined and concentrated under vacuum to provide the desired compound (P-1518, 27 mg). MS (ESI) [M+H+]+=521.95.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US09440969B2 |
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| 출처 데이터셋 | uspto-grants-2016_09 |
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| ORD ID | ord-cd9cd68d9e844acc931889fd7116d154 |
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| 출처 메모 | uspto-grants-2016_09 |
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