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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 468생성일: 2026년 10월 23일

4-(Methylsulfonyl)aniline → 4-(2,6-Dimethylpyridin-3-yloxy)-N-(4-(methylsulfonyl)phenyl)pyridin-2-amine

https://huagongshe.com/ko/reaction/468

반응식

참여 물질

역할이름HCID투입량
반응물4-(Methylsulfonyl)anilineHCID 79617—
반응물3-(2-Chloropyridin-4-yl)oxy-2,6-dimethyl-pyridineHCID 44598200—
시약Cesium carbonateHCID 10796—
촉매1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine)HCID 636044—
촉매Palladium (II) acetateHCID 4144353—
용매DimethylacetamideHCID 31374—
생성물4-(2,6-Dimethylpyridin-3-yloxy)-N-(4-(methylsulfonyl)phenyl)pyridin-2-amineHCID 6894285850.82%

반응 조건

온도150 °C

반응 단계

In a 10 mL microwave reactor 3-(2-chloropyridin-4-yloxy)-2,6-dimethylpyridine (100 mg, 0.43 mmol) and 4-(methylsulfonyl)aniline (73.0 mg, 0.43 mmol) were dissolved in DMA (3 mL) to give a tan solution.To the resultant solution Cesium carbonate (0.068 mL, 0.85 mmol) was added and sparged with nitrogen for 1 minute. Then Palladium(II) acetate (6.70 mg, 0.03 mmol) and 9,9-Dimethyl-4,5-bis(diphenylphosphino)xanthene (29.6 mg, 0.05 mmol) were added and the reaction mixture was sealed. The reaction was heated to150 °C for 25 minutes in the biotage microwave.The reaction was cooled to room temperature and LCMS shows reaction was completed. Reaction mixture was filtered through Celite Bed and washed with Dichloromethane. Filtrate was subjected to concentration to get DMA solution which was given to analytical department to purify using Mass based HPLC. After purification compound was isolated to get pale yellow solid of 4-(2,6-dimethylpyridin-3-yloxy)-N-(4-(methylsulfonyl)phenyl)pyridin-2-amine (80 mg, 50.8 %)

출처 및 근거

출처 데이터셋750 AstraZeneca ELN dataset
ORD IDord-0a36562a530a4f6bb99c0bf4c44fc018
출처 메모750 AstraZeneca ELN dataset