Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 339692생성일: 2026년 10월 24일
Cesium carbonate → (R)-tert-butyl 1-(2-([1,2,4]triazolo[4,3-a]pyridin-3-yl)quinolin-8-yl)piperidin-3-ylcarbamate
https://huagongshe.com/ko/reaction/339692
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Cesium carbonate | HCID 10796 | — |
| 반응물 | Binap, (A+-)- | HCID 634876 | — |
| 반응물 | (3R)-3-Aminopiperidine, 3-BOC protected | HCID 1514172 | — |
| 반응물 | 2-([1,2,4]Triazolo[4,3-a]pyridin-3-yl)quinolin-8-yl trifluoromethanesulfonate | HCID 86654354 | — |
| 촉매 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 생성물 | (R)-tert-butyl 1-(2-([1,2,4]triazolo[4,3-a]pyridin-3-yl)quinolin-8-yl)piperidin-3-ylcarbamate | HCID 67234401 | 67.5% |
반응 단계
2-([1,2,4]triazolo[4,3-a]pyridin-3-yl)quinolin-8-yl trifluoromethanesulfonate (0.040 g, 0.10 mmol), (R)-tert-butyl piperidin-3-ylcarbamate (0.026 g, 0.13 mmol), cesium carbonate (0.050 g, 0.15 mmol), Pd2dba3 (0.0046 g, 0.0051 mmol) and 2,2′-bis(diphenylphosphino)-1,1′-binaphthyl(0.0063 g, 0.010 mmol) were added to minimal degassed toluene and heated in a seal vial overnight at 92° C. After stirring overnight, DCM was added, solids removed through filtration (Waters filter), and the filtrate was concentrated. The crude material was purified by flash column chromatography (gradient elution of 6% NH4 in MeOH/DCM). The desired product (30 mg) was isolated, as a 1:1 mixture with the triflate starting material. The mixture was used without further purification.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US08895550B2 |
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| 출처 데이터셋 | uspto-grants-2014_11 |
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| ORD ID | ord-66a428f051d6407180f76925f1c96d49 |
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| 출처 메모 | uspto-grants-2014_11 |
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