Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 59133생성일: 2026년 10월 24일
Cesium carbonate → N4-Methyl-N2-(4-(4-methyl-1H-imidazol-1-yl)phenyl)-6-((2,2,2-trifluoroethoxy)methyl)-pyrimidine-2,4-diamine
https://huagongshe.com/ko/reaction/59133
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Cesium carbonate | HCID 10796 | — |
| 반응물 | 2-(Dicyclohexylphosphino)biphenyl | HCID 2734216 | — |
| 반응물 | 4-(4-Methyl-1h-imidazol-1-yl)benzenamine | HCID 16005170 | — |
| 반응물 | 2-Chloro-N-methyl-6-((2,2,2-trifluoroethoxy)methyl)pyrimidin-4-amine | HCID 117821210 | — |
| 촉매 | palladium(II) acetate | HCID 167845 | — |
| 용매 | 1,4-Dioxane | HCID 31275 | — |
| 생성물 | N4-Methyl-N2-(4-(4-methyl-1H-imidazol-1-yl)phenyl)-6-((2,2,2-trifluoroethoxy)methyl)-pyrimidine-2,4-diamine | HCID 86344431 | 40.2% |
반응 단계
A mixture of 2-chloro-N-methyl-6-((2,2,2-trifluoroethoxy)methyl)pyrimidin-4-amine (85 mg, 0.33 mmol), 4-(4-methyl-1H-imidazol-1-yl)aniline (100 mg, 0.58 mmol), cesium carbonate (217 mg, 0.67 mmol), palladium(II) acetate (11 mg, 0.05 mmol) and 2-(dicyclohexylphosphino)-biphenyl (17 mg, 0.05 mmol) in dioxane (3 mL) was heated in a microwave reactor under notrogen atmosphere at 120° C. for 90 min. The reaction mixture was filtered through a pad of diatomeous earth which was eluted with MeOH. The mixture was partitioned between EtOAc and sodium hydroxide (aq, 1 M). The organic phase was separated, dried over sodium sulfate and concentrated in vacuum. The residue was purified by preparative HPLC to give the title compound as a solid 52 mg, (40%).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US09439904B2 |
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| 출처 데이터셋 | uspto-grants-2016_09 |
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| ORD ID | ord-5b10546332b64f55a15b362357df6f61 |
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| 출처 메모 | uspto-grants-2016_09 |
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