Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
Morpholine → Tert-butyl 4-((4'-chloro-4-morpholinobiphenyl-2-yl)methyl)piperazine-1-carboxylate
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | Morpholine | HCID 8083 | — |
| 반응물 | Cesium carbonate | HCID 10796 | — |
| 반응물 | 2-(Di-tert-butylphosphino)biphenyl | HCID 2734215 | — |
| 반응물 | Tert-butyl 4-((4'-chloro-4-(trifluoromethylsulfonyloxy)biphenyl-2-yl)methyl)piperazine-1-carboxylate | HCID 87315805 | — |
| 촉매 | palladium(II) acetate | HCID 167845 | — |
| 용매 | Tetrahydrofuran | HCID 8028 | — |
| 용매 | Ethyl Acetate | HCID 8857 | — |
| 생성물 | Tert-butyl 4-((4'-chloro-4-morpholinobiphenyl-2-yl)methyl)piperazine-1-carboxylate | HCID 67227322 | — |
반응 단계
A suspension of EXAMPLE 198B (500 mg), morpholine (80 mg), palladium (II) acetate (22 mg), biphenyl-2-yldi-tert-butylphosphine (50 mg) and cesium carbonate (427 mg) in anhydrous tetrahydrofuran (6 mL) was heated at 50° C. overnight. The reaction mixture was cooled to room temperature and diluted with ethyl acetate. The organic phase was washed with water, brine, dried over anhydrous sodium sulfate, filtered and concentrated. The crude material was purified by flash column purification with 30-50% ethyl acetate/hexane to afford the title compound.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US09072748B2 |
| 출처 데이터셋 | uspto-grants-2015_07 |
| ORD ID | ord-b696ee6c0a0b4912ab75d775b8be2214 |
| 출처 메모 | uspto-grants-2015_07 |