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Benzenecarboximidamide, 4-hydroxy-, hydrochloride (1:1) → 3-[5-(4-Amidinophenoxycarbonyl)thiophen-2-yl]-2-methylpropenoic acid tert-butyl ester
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Benzenecarboximidamide, 4-hydroxy-, hydrochloride (1:1) | HCID 217124 | — |
| 反応物 | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| 反応物 | 5-(2-(tert-Butoxycarbonyl)-1-propenyl)-2-thiophenecarboxylic acid | HCID 77478494 | — |
| 溶媒 | Pyridine | HCID 1049 | — |
| 生成物 | 3-[5-(4-Amidinophenoxycarbonyl)thiophen-2-yl]-2-methylpropenoic acid tert-butyl ester | HCID 86673317 | 86.3% |
反応手順
5-(2-(tert-Butoxycarbonyl)-1-propenyl)-2-thiophenecarboxylic acid (0.51 g, 1.89 mmol) and 4-hydroxybenzamidine hydrochloride (0.33 g, 1.89 mmol) were dissolved in pyridine (10 mL), WSC hydrochloride (0.54 g, 2.8 mmol) was added, and the mixture was stirred overnight. The mixture was purified by high performance liquid chromatography and freeze-dried to give the title compound (0.63 g).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09115107B2 |
| 出典データセット | uspto-grants-2015_08 |
| ORD ID | ord-cc29a6b81db1469dabc7c771c1072f24 |
| 出典メモ | uspto-grants-2015_08 |