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Water → 2-chloro-N-(6-methoxy-[1,5]naphthyridin-4-yl)-acetamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | Ethyl chloroacetate | HCID 7751 | — |
| 反応物 | 6-Methoxy-1,5-naphthyridin-4-amine | HCID 11435236 | — |
| 反応物 | Potassium tert-butoxide | HCID 23665647 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 2-chloro-N-(6-methoxy-[1,5]naphthyridin-4-yl)-acetamide | HCID 66737337 | 45% |
反応手順
To a solution of 6-methoxy-1,5-naphthyridin-4-amine (553 mg, 3.116 mmol) in THF (45 mL) was added t-BuOK (390 mg, 1.1 eq) at 0° C. The resulting brown suspension was stirred at rt for 1.5 h and then added dropwise to a solution of ethyl chloroacetate (0.337 mL, 1 eq) in THF (30 mL) at −5° C. The mixture was allowed to warm to rt and was further stirred for 3 h. Water was added and the solvent was removed under reduced pressure. The resulting precipitate was filtered and further dried at HV to afford the title intermediate as a beige solid (357 mg, 45% yield).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08114867B2 |
| 出典データセット | uspto-grants-2012_02 |
| ORD ID | ord-699dbfc4c5404fc8b9a1ae1bb6fe4f4c |
| 出典メモ | uspto-grants-2012_02 |