Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
5-Fluoroindole-2-carboxylic acid → 5-Fluoro-N-{1-[2-(7-fluoro-2-oxoquinoxalin-1(2H)-yl)ethyl]piperidin-4-yl}-1H-indole-2-carboxamide
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | 5-Fluoroindole-2-carboxylic acid | HCID 1820 | — |
| 반응물 | 1-Hydroxybenzotriazole hydrate | HCID 2796029 | — |
| 반응물 | 3-(Dimethylamino)propyl-ethyl-(iminomethylidene)azanium | HCID 21883392 | — |
| 반응물 | 1-(2-(4-aminopiperidin-1-yl)ethyl)-7-fluoroquinoxalin-2(1H)-one | HCID 59397907 | — |
| 용매 | dichloromethane N,N-dimethylformamide | HCID 22350042 | — |
| 생성물 | 5-Fluoro-N-{1-[2-(7-fluoro-2-oxoquinoxalin-1(2H)-yl)ethyl]piperidin-4-yl}-1H-indole-2-carboxamide | HCID 15983073 | 79.6% |
반응 단계
A mixture of 1-[2-(4-aminopiperidin-1-yl)ethyl]-7-fluoroquinoxalin-2(1H)-one (Intermediate 140, 130 mg, 0.448 mmol), 5-fluoro-1H-indole-2-carboxylic acid (96.3 mg, 0.538 mmol), N-(3-Dimethylaminopropyl)-N-ethylcarbodiimide (EDC)(124 mg, 0.645 mmol) and 1-Hydroxybenzotriazole hydrate (HOBT) (87 mg, 0.645 mmol) in dichloromethane/DMF (4:1, 10 mL) was stirred for 2.5 hours at room temperature. The solvent was removed under reduced pressure and the residue was suspended in methanol, stirred for 45 minutes and then filtered to give title compound (161 mg).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US07875715B2 |
| 출처 데이터셋 | uspto-grants-2011_01 |
| ORD ID | ord-113c25239d61448faf92cc47a1cf30db |
| 출처 메모 | uspto-grants-2011_01 |