Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 12793생성일: 2026년 10월 24일
Potassium Fluoride → 5-(5-chloro-2-fluoro-3-pyridinyl)-1-(3-{(1S,5R)-1-[4-(trifluoromethyl)phenyl]-3-azabicyclo[3.1.0]hex-3-yl}propyl)-2,4(1H,3H)-pyrimidinedione dihydrochloride
https://huagongshe.com/ko/reaction/12793
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Potassium Fluoride | HCID 522689 | — |
| 반응물 | 5-Chloro-2-fluoropyridine-3-boronic Acid | HCID 24901779 | — |
| 반응물 | 5-iodo-1-(3-{(1S,5R)-1-[4-(trifluoromethyl)phenyl]-3-azabicyclo[3.1.0]hex-3-yl}propyl)-2,4(1H,3H)-pyrimidinedione | HCID 67519719 | — |
| 촉매 | palladium(II) acetate | HCID 167845 | — |
| 용매 | Methanol | HCID 887 | — |
| 생성물 | 5-(5-chloro-2-fluoro-3-pyridinyl)-1-(3-{(1S,5R)-1-[4-(trifluoromethyl)phenyl]-3-azabicyclo[3.1.0]hex-3-yl}propyl)-2,4(1H,3H)-pyrimidinedione dihydrochloride | HCID 86615960 | 6% |
반응 단계
A mixture of 5-iodo-1-{3-[(1S,5R)-1-(4-trifluoromethyl-phenyl)-3-aza-bicyclo[3.1.0]hex-3-yl]-propyl}-1H-pyrimidine-2,4-dione (Prep 40, 150 mg, 0.3 mmol), 2-fluoro-5-chloropyridine-3-boronic acid (142 mg, 0.9 mmol), KF (157 mg, 2.7 mmol), and Pd(OAc)2 (20 mg) in degassed MeOH (4 ml) was placed in a microwave oven and warmed at 120° C. for 25 minutes. The mixture was filtered, MeOH was evaporated and the crude partitioned between brine and ethyl acetate. The organic phase was dried (Na2SO4) and evaporated; the crude was purified by flash chromatography with ethyl acetate-NH4OH (0.5%) to give the title compound (10 mg, 6% yield).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US07727988B2 |
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| 출처 데이터셋 | uspto-grants-2010_06 |
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| ORD ID | ord-2f63d5a76ab14a41b250ef46922cb2d2 |
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| 출처 메모 | uspto-grants-2010_06 |
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