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Triethylamine → (R)-2-(2-chloro-5-iodopyrimidine-4-ylamino)propan-1-ol
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | (R)-(-)-2-Amino-1-propanol | HCID 80308 | — |
| 反応物 | 2,4-Dichloro-5-iodopyrimidine | HCID 263438 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | (R)-2-(2-chloro-5-iodopyrimidine-4-ylamino)propan-1-ol | HCID 59550865 | 88% |
反応手順
To a solution of 2,4-dichloro-5-iodopyrimidine (3.0 g; 10.9 mol) in acetonitrile (35 mL) was added triethylamine (1.32 g, 1.82 mL, 13.1 mmol), followed by (R)-2-aminopropanol (0.88 g, 11.8 mmol). The mixture was stirred at room temperature for 24 h and was then diluted with ethyl acetate, followed by extraction with brine, 10% aqueous citric acid, and aqueous sodium bicarbonate. After drying over sodium sulfate, the solvent was evaporated and the residue was purified by column chromatography to give the title compound (3.0 g, 88% yield).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08524724B2 |
| 出典データセット | uspto-grants-2013_09 |
| ORD ID | ord-6bcc1139f9224011bd5c597b37e59a37 |
| 出典メモ | uspto-grants-2013_09 |