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3,4-Difluorophenyl isocyanate → N-(4-t-Butoxycarbonylaminothiophen-3-yl)-5-[3-(3,4-difluorophenyl)-1-[3-(morpholin-4-yl)propyl]ureidomethyl]pyridine-2-carboxylic acid amide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 3,4-Difluorophenyl isocyanate | HCID 2734708 | — |
| 反応物 | N-(4-t-butoxycarbonylaminothiophen-3-yl)-5-[3-(morpholin-4-yl)propylaminomethyl]pyridine-2-carboxylic acid amide | HCID 67049993 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | N-(4-t-Butoxycarbonylaminothiophen-3-yl)-5-[3-(3,4-difluorophenyl)-1-[3-(morpholin-4-yl)propyl]ureidomethyl]pyridine-2-carboxylic acid amide | HCID 67050108 | 92% |
反応手順
3,4-Difluorophenyl isocyanate (15 μL, 0.13 mmol) was added to a solution of N-(4-t-butoxycarbonylaminothiophen-3-yl)-5-[3-(morpholin-4-yl)propylaminomethyl]pyridine-2-carboxylic acid amide (Reference Compound No. 5-12, 43 mg, 0.091 mmol) in dichloromethane (2.0 mL), and then the reaction mixture was stirred at room temperature for 1.5 hours. The reaction solution was purified by silica gel column chromatography (chloroform-methanol) to give 53 mg of the title reference compound as a colorless solid. (Yield 92%)
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08198271B2 |
| 出典データセット | uspto-grants-2012_06 |
| ORD ID | ord-c729d5e047b94b388dc7389eadae3c71 |
| 出典メモ | uspto-grants-2012_06 |