참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Pyrazole | HCID 1048 | — |
| 반응물 | Cesium carbonate | HCID 10796 | — |
| 반응물 | 5-Amino-2-fluoropyridine | HCID 819440 | — |
| 용매 | Chloroform | HCID 6212 | — |
| 용매 | N-methyl-2-pyrrolidone | HCID 13387 | — |
| 생성물 | 6-(1H-pyrazol-1-yl)pyridin-3-amine | HCID 16774822 | 17% |
반응 단계
Commercial 6-fluoropyridin-3-amine (500 mg, 4.46 mmol) was dissolved in 20 mL dry NMP. To it were added pyrazole (910 mg, 13.4 mmol) and cesium carbonate (4.4 g, 13.4 mmol). The mixture was stirred in a sealed tube at 120° C. for over the weekend (3 nights). The mixture was diluted with chloroform, washed with brine (3 times), dried, concentrated and subjected to flash column (0 to 30% EtOAc in DCM) to isolate 6-(1H-pyrazol-1-yl)pyridin-3-amine (120 mg, 17% yield).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 특허 번호 | US08846928B2 |
|---|
| 출처 데이터셋 | uspto-grants-2014_09 |
|---|
| ORD ID | ord-b211c993c0db4887b1819cb46fe63efb |
|---|
| 출처 메모 | uspto-grants-2014_09 |
|---|
