関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | 2-(Trifluoromethoxy)benzoyl Chloride | HCID 2777241 | — |
| 反応物 | 2-Amino-4-(2-furyl)-5-(tetrahydropyran-4-ylcarbonyl)thiazole | HCID 86612468 | — |
| 触媒 | 4-(Dimethylamino)pyridine | HCID 14284 | — |
| 溶媒 | Pyridine | HCID 1049 | — |
| 生成物 | N-[4-(2-Furyl)-5-(tetrahydropyran-4-ylcarbonyl)thiazol-2-yl]-2-(trifluoromethoxy)benzamide | HCID 23144208 | 53% |
反応手順
Compound 454 (125 mg, 0.450 mmol) and DMAP (0.022 mmol) were suspended in pyridine (2 mL), and 2-(trifluoromethoxy)benzoyl chloride (202 mg, 0.900 mmol) was added thereto, followed by stirring at 80° C. for 6 hours. The reaction mixture was poured into water, followed by extraction with ethyl acetate. The organic layer was washed with a saturated aqueous solution of sodium chloride and dried over anhydrous magnesium sulfate, and then the solvent was distilled away under reduced pressure. The resulting residue was recrystallized from ethanol to afford the entitled Compound 475 (111 mg, 53%) as a pale yellow solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08889718B2 |
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| 出典データセット | uspto-grants-2014_11 |
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| ORD ID | ord-aa3505459a4e4d738412fa136f04b93c |
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| 出典メモ | uspto-grants-2014_11 |
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