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Water → 2-(2-(4-Methoxycarbonylphenylmethyl)aminonitrobenzen-5-yl)benzoxazole
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | Methyl 4-(aminomethyl)benzoate hydrochloride | HCID 2729253 | — |
| 反応物 | 2-(4-Fluoro-3-nitrophenyl)benzoxazole | HCID 21990970 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 2-(2-(4-Methoxycarbonylphenylmethyl)aminonitrobenzen-5-yl)benzoxazole | HCID 67498451 | 95.3% |
反応手順
To a suspension of 2-(4-fluoro-3-nitrophenyl)benzoxazole (see Working Example 15-2) (250 mg, 0.968 mmol) in acetonitrile (5 mL) was added triethylamine (245 mg, 2.42 mmol) and 4-carbomethoxybenzylamine hydrochloride (215 mg, 1.07 mmol), and this was heated to reflux for 2 hours. After the reaction was complete, this was cooled to room temperature, water was added, and after the precipitated crystals were filtered and washed with water, they were dried to yield the title compound (372 mg, 95% yield).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08829035B2 |
| 出典データセット | uspto-grants-2014_09 |
| ORD ID | ord-4edf92dcebf1480ca969c2aa9d0f382b |
| 出典メモ | uspto-grants-2014_09 |