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1-Hydroxybenzotriazole → Rac-2-(3-cyclopropyl-2-oxo-4-phenyl-2,3-dihydro-1h-imidazol-1-yl)-n-[1'-(2-naphthyl)ethyl]-acetamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1-Hydroxybenzotriazole | HCID 75771 | — |
| 反応物 | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| 反応物 | 1-(Naphthalen-2-yl)ethan-1-amine | HCID 3857145 | — |
| 反応物 | (3-cyclopropyl-2-oxo-4-phenyl-2,3-dihydro-1H-imidazol-1-yl)-acetic acid | HCID 58011929 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | Rac-2-(3-cyclopropyl-2-oxo-4-phenyl-2,3-dihydro-1h-imidazol-1-yl)-n-[1'-(2-naphthyl)ethyl]-acetamide | HCID 58012213 | — |
反応手順
40 mg (0.155 mmol) of (3-cyclopropyl-2-oxo-4-phenyl-2,3-dihydro-1H-imidazol-1-yl)-acetic acid from Example 128A, 29.2 mg (0.17 mmol) of 1-(2-naphthyl)ethylamine, 38.6 mg (0.20 mmol) of EDC hydrochloride and 25.1 mg (0.19 mmol) of HOBt are dissolved in 1.5 ml of dry DMF and stirred overnight at RT. The crude product is purified by preparative HPLC [Method 10, with addition of 0.01 M hydrochloric acid in the water]. The target compound is obtained in a yield of 41 mg (63% of theory).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08084481B2 |
| 出典データセット | uspto-grants-2011_12 |
| ORD ID | ord-2be96ec387e743edbb9035ea628c9eb1 |
| 出典メモ | uspto-grants-2011_12 |