Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 59150생성일: 2026년 10월 23일
Cesium carbonate → 4-(Azetidin-1-yl)-N-(3-methoxy-4-(6-methylpyridazin-4-yl)phenyl)-6-((2,2,2-trifluoroethoxy)methyl)pyrimidin-2-amine
https://huagongshe.com/ko/reaction/59150
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Cesium carbonate | HCID 10796 | — |
| 반응물 | 2-(Dicyclohexylphosphino)biphenyl | HCID 2734216 | — |
| 반응물 | 3-Methoxy-4-(6-methylpyridazin-4-yl)aniline | HCID 66859066 | — |
| 반응물 | 4-(Azetidin-1-yl)-2-chloro-6-((2,2,2-trifluoroethoxy)methyl)pyrimidine | HCID 117821136 | — |
| 촉매 | palladium(II) acetate | HCID 167845 | — |
| 용매 | 1,4-Dioxane | HCID 31275 | — |
| 생성물 | 4-(Azetidin-1-yl)-N-(3-methoxy-4-(6-methylpyridazin-4-yl)phenyl)-6-((2,2,2-trifluoroethoxy)methyl)pyrimidin-2-amine | HCID 86344803 | 29% |
반응 단계
A mixture of 4-(azetidin-1-yl)-2-chloro-6-((2,2,2-trifluoroethoxy)methyl)pyrimidine (30 mg, 0.11 mmol), 3-methoxy-4-(6-methylpyridazin-4-yl)aniline (23 mg, 0.11 mmol), cesium carbonate (69 mg, 0.21 mmol), palladium(II) acetate (4 mg, 0.02 mmol) and 2-(dicyclohexyl-phosphino)biphenyl (6 mg, 0.02 mmol) in dioxane (2 mL) was heated under argon at 120° C. for 90 minutes in a microwave reactor. The mixture was filtered through a short silica plug which was washed with 10% solution of methanol in EtOAc (75 mL). The eluate was concentrated and the residue was purified by preparative HPLC to give the title compound as a solid 14 mg (29%).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 특허 번호 | US09439904B2 |
|---|
| 출처 데이터셋 | uspto-grants-2016_09 |
|---|
| ORD ID | ord-48f99684d7fa44bea30d5c7071317a2a |
|---|
| 출처 메모 | uspto-grants-2016_09 |
|---|