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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 675생성일: 2026년 10월 24일

5-Chloro-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidine-3-carbonitrile → N-[5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]-2-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]phenyl]acetamide

https://huagongshe.com/ko/reaction/675

반응식

참여 물질

역할이름HCID투입량
반응물5-Chloro-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidine-3-carbonitrileHCID 89827173—
반응물N-[5-amino-2-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]phenyl]acetamideHCID 166477480—
시약Cesium carbonateHCID 10796—
촉매1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine)HCID 636044—
촉매Bis(dibenzylideneacetone)palladiumHCID 9811564—
용매DimethylacetamideHCID 31374—
생성물N-[5-[[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino]-2-[(3S)-3-(dimethylamino)pyrrolidin-1-yl]phenyl]acetamideHCID 12704553836.66%

반응 조건

온도150 °C

반응 단계

in microwave tube was 5-chloro-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidine-3-carbonitrile (100mg, 0.43 mmol), [Reactants], and (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (24.76 mg, 0.04 mmol) in DMA (1.0 mL).Pd2(dba)3 (19.60 mg, 0.02 mmol) and cesium carbonate (279 mg, 0.86 mmol) were added. degassed, filled with N2.capped. then microwave 150C for 30 min. filtered, then concentrated. The crude material was purified by ISC(Hex to Hex:EtOAc=1;1 to EtOAc to EtOAc:MeOH=10:1 to EtOAc:MeOH:Et3N=10:1:0.1)) to give no very pure product. collect the product fraction, concentrated to dryness. no pure enough, tried to form solid. it failed sent to ananlytic group for purification. came back. it was OK 1TFA salt. NMR LCMS are OK

출처 및 근거

출처 데이터셋750 AstraZeneca ELN dataset
ORD IDord-6ca842b2903f47c19f42752e7a96ea52
출처 메모750 AstraZeneca ELN dataset