Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
4-Methylmorpholine → 6-Cyclopropyl-3-(pyrimidin-5-ylamino)-pyrazine-2-carboxylic acid [4-(2-isopropoxy-ethylcarbamoyl)-pyridin-3-yl]-amide
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | 4-Methylmorpholine | HCID 7972 | — |
| 반응물 | 2-(Propan-2-yloxy)ethan-1-amine | HCID 533866 | — |
| 반응물 | Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1) | HCID 9886157 | — |
| 반응물 | 3-{[6-Cyclopropyl-3-(pyrimidin-5-ylamino)-pyrazine-2-carbonyl]-amino}-isonicotinic acid | HCID 70098928 | — |
| 용매 | Tetrahydrofuran | HCID 8028 | — |
| 생성물 | 6-Cyclopropyl-3-(pyrimidin-5-ylamino)-pyrazine-2-carboxylic acid [4-(2-isopropoxy-ethylcarbamoyl)-pyridin-3-yl]-amide | HCID 58548177 | 80.4% |
반응 단계
To a stirred mixture of 2-aminoethyl isopropyl ether (25 mg, 242 μmol) and 3-{[6-cyclopropyl-3-(pyrimidin-5-ylamino)-pyrazine-2-carbonyl]-amino}-isonicotinic acid (101 mg, 267 μmol) at rt in THF (5 ml) under an argon atmosphere were added 4-methylmorpholine (123 mg, 134 μl, 1.21 mmol) and HATU (184 mg, 485 μmol). The mixture was heated to reflux and stirring was continued for 1 day. The reaction mixture was concentrated. The crude product was purified by silica gel chromatography using an EtOAc/MeOH gradient as eluent. After trituration with MeOH, the title compound (90 mg, 80%) was obtained as yellow solid.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US08623866B2 |
| 출처 데이터셋 | uspto-grants-2014_01 |
| ORD ID | ord-b4c10af434614ecbaae0174a684336ff |
| 출처 메모 | uspto-grants-2014_01 |