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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 546579생성일: 2026년 10월 25일

Cesium carbonate → (2R)-2-amino-N-{5-[3-({2-[(dimethylcarbamoyl)amino]pyridin-4-yl}methyl)-4,4-dimethyl-2,5-dioxoimidazolidin-1-yl]-2-(trifluoromethoxy)phenyl}-2-phenylacetamide

https://huagongshe.com/reaction/546579

반응식

참여 물질

역할이름HCID투입량
반응물Cesium carbonateHCID 10796—
반응물N,N-DimethylureaHCID 11737—
반응물(9,9-dimethyl-9H-xanthene-3,6-diyl)bis(diphenylphosphine)HCID 86628973—
반응물(2R)-2-amino-N-[5-{3-[(2-chloropyridin-4-yl)methyl]-4,4-dimethyl-2,5-dioxoimidazolidin-1-yl}-2-(trifluoromethoxy)phenyl]-2-phenylacetamideHCID 86629090—
촉매palladium(II) acetateHCID 167845—
용매1,4-DioxaneHCID 31275—
생성물(2R)-2-amino-N-{5-[3-({2-[(dimethylcarbamoyl)amino]pyridin-4-yl}methyl)-4,4-dimethyl-2,5-dioxoimidazolidin-1-yl]-2-(trifluoromethoxy)phenyl}-2-phenylacetamideHCID 57626026—

반응 조건

온도40 °C

반응 단계

To a solution of 150 mg of (2R)-2-amino-N-[5-{3-[(2-chloropyridin-4-yl)methyl]-4,4-dimethyl-2,5-dioxoimidazolidin-1-yl}-2-(trifluoromethoxy)phenyl]-2-phenylacetamide obtained in stage d) of Example 5a in 10 mL of dioxane are successively added, under argon, 30 mg of N,N-dimethylurea, 13 mg of (9,9-dimethyl-9H-xanthene-3,6-diyl)bis(diphenylphosphine) (Xantphos), 5 mg of palladium acetate and 280 mg of caesium carbonate. The reaction mixture is refluxed for 1 hour and then filtered, and the filtrate is concentrated under reduced pressure. The residue is taken up in 10 mL of dioxane, 5 mL of a 4N solution of hydrogen chloride in dioxane are then added and the reaction mixture is stirred at 40° C. for 1 hour. After concentrating under reduced pressure, the residue is purified by HPLC (gradient: water/acetonitrile containing 0.1% formic acid) to give 45 mg of ((2R)-2-amino-N-{5-[3-({2-[(dimethylcarbamoyl)amino]pyridin-4-yl}methyl)-4,4-dimethyl-2,5-dioxoimidazolidin-1-yl]-2-(trifluoromethoxy)phenyl}-2-phenylacetamide, the characteristics of which are as follows:

출처 및 근거

DOI10.6084/m9.figshare.5104873.v1
특허 번호US07935819B2
출처 데이터셋uspto-grants-2011_05
ORD IDord-0885919cbf884530850917315bd0d9bb
출처 메모uspto-grants-2011_05