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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

반응식

참여 물질

역할이름HCID투입량
반응물Potassium FluorideHCID 522689—
반응물5-Chloro-2-fluoropyridine-3-boronic AcidHCID 24901779—
반응물5-iodo-1-(3-{(1S,5R)-1-[4-(trifluoromethyl)phenyl]-3-azabicyclo[3.1.0]hex-3-yl}propyl)-2,4(1H,3H)-pyrimidinedioneHCID 67519719—
촉매palladium(II) acetateHCID 167845—
용매MethanolHCID 887—
생성물5-(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 dihydrochlorideHCID 866159606%

반응 조건

온도120 °C

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

DOI10.6084/m9.figshare.5104873.v1
특허 번호US07727988B2
출처 데이터셋uspto-grants-2010_06
ORD IDord-2f63d5a76ab14a41b250ef46922cb2d2
출처 메모uspto-grants-2010_06