Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 747235생성일: 2026년 10월 26일
Tris(furan-2-yl)phosphane → (5R)-3-{4'-[5-({[tert-butyl(dimethyl)silyl]oxy}methyl)-4,5-dihydroisoxazol-3-yl]-1,1'-biphenyl-4-yl}-5-[(4-methyl-1H-1,2,3-triazol-1-yl)methyl]-1,3-oxazolidin-2-one
https://huagongshe.com/reaction/747235
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Tris(furan-2-yl)phosphane | HCID 521585 | — |
| 반응물 | 5-({[tert-Butyl(dimethyl)silyl]oxy}methyl)-3-[4-(trimethylstannyl)phenyl]4,5-dihydroisoxazole | HCID 59749429 | — |
| 반응물 | (5R)-3-(4-Iodophenyl)-5-[(4-methyl-1H-1,2,3-triazol-1-yl)methyl]-1,3-oxazolidin-2-one | HCID 59749434 | — |
| 촉매 | Tris(dibenzylideneacetone) palladium | HCID 44556509 | — |
| 용매 | 1,4-Dioxane | HCID 31275 | — |
| 생성물 | (5R)-3-{4'-[5-({[tert-butyl(dimethyl)silyl]oxy}methyl)-4,5-dihydroisoxazol-3-yl]-1,1'-biphenyl-4-yl}-5-[(4-methyl-1H-1,2,3-triazol-1-yl)methyl]-1,3-oxazolidin-2-one | HCID 59749445 | 28.3% |
반응 단계
5-({[tert-Butyl(dimethyl)silyl]oxy}methyl)-3-[4-(trimethylstannyl)phenyl]4,5-dihydroisoxazole (0.70 g, 1.6 mmol), (5R)-3-(4-iodophenyl)-5-[(4-methyl-1H-1,2,3-triazol-1-yl)methyl]-1,3-oxazolidin-2-one (0.5 g, 1.29 mmol), tri-2-furyl phosphine (0.06 g, 0.26 mmol) and tris(dibenzylideneacetone)palladium (0) (0.12 g, 0.13 mmol) were dissolved in 1,4-dioxane (5 ml) and degassed three times. The mixture was then heated to 90° C. and stirred for 18 hr. LCMS indicated that the reaction was not yet complete, so it was cooled and an additional (0.12 g, 0.13 mmol) of tris(dibenzylidene acetone) palladium (0) was added, the mixture degassed and reheated to 110° C. for 3 hours, and 25° C. for 40 hours. The solution was concentrated in vacuo and purified by silica flash chromatography with 5-10% methanol in dichloromethane as eluent giving 0.2 g of the desired product as a yellow solid.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US07396847B2 |
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| 출처 데이터셋 | uspto-grants-2008_07 |
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| ORD ID | ord-aa766d7d8b7b4900aa80758113d2bce9 |
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| 출처 메모 | uspto-grants-2008_07 |
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