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
참여 물질
| 역할 | 이름 | HCID | 투입량 |
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| 반응물 | Sulfur, trifluoro(N-methylmethanaminato)- | HCID 123203 | — |
| 반응물 | 9-(1-hydroxy-2-morpholinoethyl)-6-(4-methoxybenzyl)pyrido[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-one | HCID 72706324 | — |
| 용매 | Acetonitrile | HCID 6342 | — |
| 용매 | Sodium Bicarbonate | HCID 516892 | — |
| 생성물 | 9-(1-fluoro-2-morpholinoethyl)-6-(4-methoxybenzyl)pyrido[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-one | HCID 86705396 | 22.8% |
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
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US09175010B2 |
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| 출처 데이터셋 | uspto-grants-2015_11 |
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| ORD ID | ord-ab221ffb96ac49afa79b31d73c725821 |
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| 출처 메모 | uspto-grants-2015_11 |
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