Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
Triethylamine → (E)-3-(4-Bromophenyl)-N-(1-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-1H-indazol-5-yl)acrylamide
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | Triethylamine | HCID 8471 | — |
| 반응물 | 1-Hydroxybenzotriazole | HCID 75771 | — |
| 반응물 | (2E)-3-(4-bromophenyl)prop-2-enoic acid | HCID 737158 | — |
| 반응물 | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| 반응물 | (5-Amino-1H-indazol-1-yl)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ol | HCID 68644438 | — |
| 용매 | Tetrahydrofuran | HCID 8028 | — |
| 생성물 | (E)-3-(4-Bromophenyl)-N-(1-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-1H-indazol-5-yl)acrylamide | HCID 68644788 | — |
반응 단계
To a solution, of (E)-3-(4-bromophenyl)acrylic acid (0.034 g, 0.15 mmol) in tetrahydrofuran (1 ml) were added 1-hydroxybenzotriazole (0.023 g, 0.17 mmol) and 1-[3-(dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride (0.032 g, 0.17 mmol). Then triethylamine (0.045 ml, 0.32 mmol) was slowly added at 0° C., followed by stirring the reaction mixture for 30 min. After the addition of (5-Amino-1H-indazol-1-yl)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ol (0.057 g, 0.15 mmol) and 4-N,N-dimethylaminopyridine (0.004 g, 0.03 mmol), stirring at room temperature for 2 hours and concentrated by evaporation in a vacuum condition. The crude product was purified by chromatography on silica gel to give the title compound.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US07812045B2 |
| 출처 데이터셋 | uspto-grants-2010_10 |
| ORD ID | ord-c4c96a3e664e4c379dc799aefdcf6148 |
| 출처 메모 | uspto-grants-2010_10 |