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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 469생성일: 2026년 10월 23일

Benzenesulfonamide, 4-amino-N-[2-(4-morpholinyl)ethyl]- → 4-[4-(2,6-Dimethylpyridin-3-yloxy)pyridin-2-ylamino]-N-(2-morpholinoethyl)benzenesulfonamide

https://huagongshe.com/ko/reaction/469

반응식

참여 물질

역할이름HCID투입량
반응물Benzenesulfonamide, 4-amino-N-[2-(4-morpholinyl)ethyl]-HCID 120569—
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-[4-(2,6-Dimethylpyridin-3-yloxy)pyridin-2-ylamino]-N-(2-morpholinoethyl)benzenesulfonamideHCID 6894667760.66%

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-amino-N-(2-morpholinoethyl)benzenesulfonamide (122 mg, 0.43 mmol) were dissolved in DMA (5 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-(4-(2,6-dimethylpyridin-3-yloxy)pyridin-2-ylamino)-N-(2-morpholinoethyl)benzenesulfonamide (125 mg, 60.7 %)

출처 및 근거

출처 데이터셋750 AstraZeneca ELN dataset
ORD IDord-7897aa67f78748769844b414acdceeae
출처 메모750 AstraZeneca ELN dataset