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Hydrochloric Acid → N-[5-(2,3,4,5-tetrahydro-1,4-benzoxazepin-7-yl)-1,3-thiazol-2-yl]acetamide hydrochloride
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Hydrochloric Acid | HCID 313 | — |
| 反応物 | tert-butyl 7-[2-(acetylamino)-1,3-thiazol-5-yl]-2,3-dihydro-1,4-benzoxazepine-4(5H)-carboxylate | HCID 59604271 | — |
| 溶媒 | Methanol | HCID 887 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | N-[5-(2,3,4,5-tetrahydro-1,4-benzoxazepin-7-yl)-1,3-thiazol-2-yl]acetamide hydrochloride | HCID 86647837 | 88% |
反応手順
A solution of 1,1-dimethylethyl 7-[2-(acetylamino)-1,3-thiazole-5-yl]-2,3-dihydro-1,4-benzoxazepine-4(5H)-carboxylate (300 mg, 0.77 mmol) in a mixture of methanol (2 mL) and 4 N hydrogen chloride in dioxane (2 mL) was refluxed for 1 min. After cooling to room temperature the reaction mixture was concentrated, and azeotroped with methanol (3×) to give N-[5-(2,3,4,5-tetrahydro-1,4-benzoxazepin-7-yl)-1,3-thiazol-2-yl]acetamide hydrochloride (221 mg, 88% yield) as a colorless solid. MS (EI) for C14H15N3O2S: 290 (MH+).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08648066B2 |
| 出典データセット | uspto-grants-2014_02 |
| ORD ID | ord-12b8f502ed634899acdc9f1d54092306 |
| 出典メモ | uspto-grants-2014_02 |