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1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → N-(3,4,5-Trimethoxyphenyl) 3-(5-Methyl-3-(2-fluoro-phenyl)isoxazol-4-oyl)aminophenyl Acetamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide | HCID 15908 | — |
| 反応物 | HCID 18756260 | HCID 18756260 | — |
| 反応物 | Methyl 3-(2-fluorophenyl)-5-methylisoxazole-4-carboxylate | HCID 18756272 | — |
| 触媒 | 4-(Dimethylamino)pyridine | HCID 14284 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | N-(3,4,5-Trimethoxyphenyl) 3-(5-Methyl-3-(2-fluoro-phenyl)isoxazol-4-oyl)aminophenyl Acetamide | HCID 59119375 | 62% |
反応手順
To a solution of 4-methoxycarbonyl-5-methyl-3-(2-fluorophenyl)isoxazole (1.00 g, 4.52 mmol) in CH2Cl2 (30 ml) was added EDCI (1.51 g, 9.04 mmol), DMAP (0.11 g, 0.90 mmol), and 2-(3-aminophenyl)-N-(3,4,5-trimethoxyphenyl)acetamide (1.70 g, 5.42 mmol). The reaction was allowed to stir for 6 h then applied to a silica gal column eluting first CH2Cl2 with followed by 10% acetone in CH2Cl2 to give the title compound (1.44 g, 62%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06670373B1 |
| 出典データセット | uspto-grants-2003_12 |
| ORD ID | ord-64a2ecb7eb564e76a9891605b47c3b09 |
| 出典メモ | uspto-grants-2003_12 |