Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 448571생성일: 2026년 10월 24일
Cesium carbonate → 4-[6-(5-Methanesulfonyl-2,3-dihydro-indol-1-yl)-5-methoxy-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester
https://huagongshe.com/ko/reaction/448571
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Cesium carbonate | HCID 10796 | — |
| 반응물 | Tri-tert-butylphosphine tetrafluoroborate | HCID 2734635 | — |
| 반응물 | 5-(Methanesulfonyl)-2,3-dihydro-1H-indole | HCID 2736136 | — |
| 반응물 | Isopropyl 4-[(6-chloro-5-methoxypyrimidin-4-yl)oxy]piperidine-1-carboxylate | HCID 51050526 | — |
| 촉매 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 용매 | 1,4-Dioxane | HCID 31275 | — |
| 생성물 | 4-[6-(5-Methanesulfonyl-2,3-dihydro-indol-1-yl)-5-methoxy-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester | HCID 25261148 | — |
반응 단계
A mixture of 8a (49 mg, 0.15 mmol), cesium carbonate (0.11 g, 2 eq), 5-Methanesulfonyl-2,3-dihydro-1H-indole (35 mg, 1.2 eq), tris(dibenzylideneacetone)-dipalladium (31 mg, 0.1 eq), tri-t-butylphosphonium tetrafluoroborate (37 mg, 0.8 eq) and dioxane (1.5 mL) was heated at 90° C. for 4 h. The mixture cooled to room temperature, dioxane was added and the mixture was filtered and washed with DCM. The filtrate was concentrated under a stream of nitrogen and the residue was taken up in 1 mL of THF and was purified by preparative HPLC to afford 8-1; LCMS 491.2 (MH+), tR=5.35 (Method 6). EC50: 201 nM.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US08481731B2 |
|---|
| 출처 데이터셋 | uspto-grants-2013_07 |
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| ORD ID | ord-653be0dfc5924825b24740bb09feb911 |
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| 출처 메모 | uspto-grants-2013_07 |
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