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Water → 2-Chloro-6-(2,4-difluoro-phenoxy)-quinazoline
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | 2-Amino-2-ethyl-1,3-propanediol | HCID 8282 | — |
| 反応物 | 2-Chloro-6-(2,4-difluoro-phenoxy)-quinazolin-4-ylamine | HCID 58905130 | — |
| 溶媒 | N-methyl-2-pyrrolidone | HCID 13387 | — |
| 生成物 | 2-Chloro-6-(2,4-difluoro-phenoxy)-quinazoline | HCID 58905137 | 60.3% |
反応手順
Compound (1G) (250 mg, 0.85 mmol) and 2-amino-2-ethyl-1,3-propanediol (298 mg, 2.5 mmol) in NMP (0.25 mL) were stirred at 120° C. for 4 h. After cooling to room temperature, the reaction mixture was poured into water and extracted with EtOAc (2×25 mL). The combined organic layers were dried over sodium sulfate and evaporated in vacuo. The crude product was purified by chromatography (silica gel, CH2Cl2: MeOH, 95:5) to afford 150 mg of the above-titled compound (Example 1). Mp=110-112.9° C. MW (M+H)+=376.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07238698B2 |
| 出典データセット | uspto-grants-2007_07 |
| ORD ID | ord-2babf05be6bd4834bda86386d146613a |
| 出典メモ | uspto-grants-2007_07 |