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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 707483생성일: 2026년 10월 26일

Sulfur, trifluoro(N-methylmethanaminato)- → 9-(1-fluoro-2-morpholinoethyl)-6-(4-methoxybenzyl)pyrido[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-one

https://huagongshe.com/reaction/707483

반응식

참여 물질

역할이름HCID투입량
반응물Sulfur, trifluoro(N-methylmethanaminato)-HCID 123203—
반응물9-(1-hydroxy-2-morpholinoethyl)-6-(4-methoxybenzyl)pyrido[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-oneHCID 72706324—
용매AcetonitrileHCID 6342—
용매Sodium BicarbonateHCID 516892—
생성물9-(1-fluoro-2-morpholinoethyl)-6-(4-methoxybenzyl)pyrido[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-oneHCID 8670539622.8%

반응 조건

온도60 °C

반응 단계

(Dimethylamino)sulfur trifluoride (0.010 ml, 0.18 mmol) was added to a stirred solution of 9-(1-hydroxy-2-morpholinoethyl)-6-(4-methoxybenzyl)pyrido[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-one (49 mg, 0.090 mmol) in acetonitrile (1 ml). After 4 hours, additional (dimethylamino)sulfur trifluoride (0.035 ml, 0.36 mmol) was added and the mixture was stirred at 60° C. for 20 hours, cooled to room temperature, diluted with aqueous sodium bicarbonate (3 mL) and extracted with DCM (2×3 mL). The combined extracts were concentrated under a stream of nitrogen and the residue was taken up in methanol, filtered and purified by preparative HPLC. The resulting material retained some impurities so it was diluted with aqueous sodium bicarbonate (3 mL) and extracted with DCM (2×3 mL). The combined extracts were concentrated under a stream of nitrogen and the residue was purified by flash chromatography (elution with 0-40% IPA in ethyl acetate) to afford 9 mg (21%) of 269 as a white powder.

출처 및 근거

DOI10.6084/m9.figshare.5104873.v1
특허 번호US09175010B2
출처 데이터셋uspto-grants-2015_11
ORD IDord-ab221ffb96ac49afa79b31d73c725821
출처 메모uspto-grants-2015_11