関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | (R)-2-Amino-2-(4-fluorophenyl)ethanol | HCID 10583003 | — |
| 反応物 | 2-chloro-N-(5-cyclopropyl-1H-pyrazol-3-yl)-6-methyl-5-nitropyrimidin-4-amine | HCID 86621765 | — |
| 溶媒 | 1-Butanol | HCID 263 | — |
| 生成物 | HCID 66589226 | HCID 66589226 | 93% |
反応手順
A solution of 2-chloro-N-(5-cyclopropyl-1H-pyrazol-3-yl)-6-methyl-5-nitropyrimidin-4-amine (Method 75; 1.0 g, 3.4 mmol), DIEA (0.57 g, 4.4 mmol), and (R)-2-amino-2-(4-fluorophenyl)ethanol (0.58 g, 3.7 mmol) in n-BuOH (15 ml) was heated to 60° C. for 2 hours. The reaction was then cooled to 25° C., concentrated, and treated with hexane. The resulting solid was collected by filtration to give the title compound (1.3 g, 93%). MS: Calcd.: 413; Found: [M+H]+ 414.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08129403B2 |
|---|
| 出典データセット | uspto-grants-2012_03 |
|---|
| ORD ID | ord-bb9368c75c0e41079420435559a39167 |
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| 出典メモ | uspto-grants-2012_03 |
|---|
