돌아가기
Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 197생성일: 2026년 10월 23일

2-amino-6-methoxy-N-methylbenzamide → 2-(2-(1,3-dimethyl-1H-pyrazol-5-ylamino)-5-(trifluoromethyl)pyridin-4-ylamino)-6-methoxy-N-methylbenzamide

https://huagongshe.com/ko/reaction/197

반응식

참여 물질

역할이름HCID투입량
반응물2-amino-6-methoxy-N-methylbenzamideHCID 12264820—
반응물N-(1,3-dimethylpyrazol-5-yl)-4-iodo-5-(trifluoromethyl)pyridin-2-amineHCID 67075489—
시약Cesium carbonateHCID 10796—
촉매1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine)HCID 636044—
촉매Palladium (II) acetateHCID 4144353—
용매1,4-DioxaneHCID 31275—
생성물2-(2-(1,3-dimethyl-1H-pyrazol-5-ylamino)-5-(trifluoromethyl)pyridin-4-ylamino)-6-methoxy-N-methylbenzamideHCID 5695129141.58%

반응 조건

온도95 °C

반응 단계

2-amino-6-methoxy-N-methylbenzamide (19.45 g, 107.95 mmol), N-(1,3-dimethyl-1H-pyrazol-5-yl)-4-iodo-5-(trifluoromethyl)pyridin-2-amine (27.5 g, 71.97 mmol) (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (4.16 g, 7.20 mmol) diacetoxypalladium (0.808 g, 3.60 mmol) and cesium carbonate (42.2 g, 129.54 mmol) were suspended in dioxane (300 mL). The reaction was degased, purged with argon sereval times and heated to 95 °C overnight. The reaction mixture was allowed to cool to rt, the insolubles were removed by filtration, washed with EtOAc and the filtrate was concentrated. The resulting residue was triturated with dichloromethane (150 ml), filtered, washed with DCM to give EN03299-47-01 (8.5 g, 19.57 mmol, 27.2 %) The filtrate was purified by flash chromatography on silica gel eluting with AcOEt and 5% methanol in ethyl acetate. Solvent were evaporated. The resulting precipitate was collected by filtration, washed with dichloromethane and dried to afford EN03299-47-02 (4.5 g, 10.36 mmol, 14.39 %). Not enought combined with _EN03299-49_

출처 및 근거

출처 데이터셋750 AstraZeneca ELN dataset
ORD IDord-62ffd954c4be4ad5b0533c19b263b236
출처 메모750 AstraZeneca ELN dataset