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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 546574생성일: 2026년 10월 25일

3-Aminopyridine → (2R)-2-amino-N-{5-(4,4-dimethyl-2,5-dioxo-3-{[2-(pyridin-3-ylamino)pyridin-4-yl]methyl}imidazolidin-1-yl)-2-[(trifluoromethyl)thio]phenyl}-2-phenylacetamide

https://huagongshe.com/reaction/546574

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참여 물질

역할이름HCID투입량
반응물3-AminopyridineHCID 10009—
반응물Cesium carbonateHCID 10796—
반응물HCID 57625996HCID 57625996—
반응물(9,9-dimethyl-9H-xanthene-3,6-diyl)bis(diphenylphosphine)HCID 86628973—
촉매palladium(II) acetateHCID 167845—
용매1,4-DioxaneHCID 31275—
생성물(2R)-2-amino-N-{5-(4,4-dimethyl-2,5-dioxo-3-{[2-(pyridin-3-ylamino)pyridin-4-yl]methyl}imidazolidin-1-yl)-2-[(trifluoromethyl)thio]phenyl}-2-phenylacetamideHCID 5762599318.7%

반응 조건

온도110 °C

반응 단계

To a solution of 33 mg of (2R)—N-(5-{3-[(2-chloropyridin-4-yl)methyl]-4,4-dimethyl-2,5-dioxoimidazolidin-1-yl}-2-[(trifluoromethyl)thio]phenyl)-2-[(9H-fluoren-9-ylacetyl)-amino]-2-phenylacetamide obtained in stage e) below in 1 mL of dioxane are successively added, under argon, 14 mg of 3-aminopyridine, 3 mg of (9,9-dimethyl-9H-xanthene-3,6-diyl)bis(diphenylphosphine) (Xantphos), 1.1 mg of palladium acetate and 61 mg of caesium carbonate. The reaction mixture is heated at 110° C. for 3 h, filtered and washed with twice 10 mL of dioxane, and the filtrate is then concentrated under reduced pressure. The residue is purified by HPLC (gradient: water/acetonitrile containing 0.1% formic acid) to give 5 mg of (2R)-2-amino-N-{5-(4,4-dimethyl-2,5-dioxo-3-{[2-(pyridin-3-ylamino)pyridin-4-yl]methyl}imidazolidin-1-yl)-2-[(trifluoromethyl)thio]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-33baa980e60e4924a399c02ff955abce
출처 메모uspto-grants-2011_05