関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 2,6-Dichloro-5-fluoro-3-pyridinecarbonitrile | HCID 2733849 | — |
| 反応物 | 3-cyclopropyl-1H-pyrazol-5-amine | HCID 2758014 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 2-chloro-6-(5-cyclopropyl-1H-pyrazol-3-ylamino)-5-fluoronicotinonitrile | HCID 86620602 | 73% |
反応手順
A solution of 5-cyclopropyl-1H-pyrazol-3-amine (1.9 g, 16.0 mmol) in CH3CN (20 ml) was added dropwise to a solution of 2,6-dichloro-5-fluoronicotinonitrile (3.0 g, 16.0 mmol) and triethylamine (2.1 g, 20.0 mmol) in CH3CN (80 ml) at 25° C. The resulting solution was then heated to 82° C. for 18 hrs, and then cooled to 25° C., at which point the product precipitated from solution. The resulting solid was filtered, and washed with CH3CN (100 ml) to give the title compound (3.2 g, 73%). MS: Calcd.: 277. Found: [M+H]+ 278.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08835465B2 |
|---|
| 出典データセット | uspto-grants-2014_09 |
|---|
| ORD ID | ord-d477f2d67dd042bbaa2cb21266ee55a9 |
|---|
| 出典メモ | uspto-grants-2014_09 |
|---|
