Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
Morpholine → 4-(4-(Tetramethyl-1,3,2-dioxaborolan-2-yl)benzoyl)morpholine
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | Morpholine | HCID 8083 | — |
| 반응물 | Triethylamine | HCID 8471 | — |
| 반응물 | 1-Hydroxybenzotriazole | HCID 75771 | — |
| 반응물 | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| 반응물 | 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzoic acid | HCID 2734621 | — |
| 용매 | Dichloromethane | HCID 6344 | — |
| 용매 | Water ethylacetate | HCID 22728543 | — |
| 생성물 | 4-(4-(Tetramethyl-1,3,2-dioxaborolan-2-yl)benzoyl)morpholine | HCID 2760141 | 81% |
반응 단계
To a solution of 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoic acid (200 mg, 0.806 mmol) in CH2Cl2 (10 mL) was subsequently added EDCl (232 mg, 1.21 mmol), HOBt (163 mg, 1.21 mmol), morpholine (0.11 mL, 1.21 mmol), and Et3N (0.22 mL, 1.61 mmol). The mixture was stirred at room temperature overnight, treated with EtOAc/H2O, and extracted with EtOAc. The combined extracts were washed with brine, dried over anhydrous Na2SO4, filtered, and concentrated. The residue was purified by flash chromatography to give the title compound (207 mg, 81% yield). MS (m/z): 318 (M+H)+
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US09434726B2 |
| 출처 데이터셋 | uspto-grants-2016_09 |
| ORD ID | ord-bfb0987f2d5d40db82adaa469c290a0e |
| 출처 메모 | uspto-grants-2016_09 |