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Cesium carbonate → N-[6-(2-fluoro-4-nitrophenoxy)[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | 1,2-Difluoro-4-nitrobenzene | HCID 123053 | — |
| 反応物 | N-(6-hydroxy[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide | HCID 57749397 | — |
| 溶媒 | Dimethyl Sulfoxide | HCID 679 | — |
| 生成物 | N-[6-(2-fluoro-4-nitrophenoxy)[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide | HCID 58158626 | 46% |
反応手順
To a solution of N-(6-hydroxy[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide (2 g, 9.16 mmol) and 1,2-difluoro-4-nitrobenzene (1.46 g, 9.16 mmol) in dimethyl sulfoxide (20 mL) was added cesium carbonate (4.48 g, 13.7 mmol), and the mixture was stirred at room temperature for 17 hr. The reaction mixture was filtered through celite, and the filtrate was diluted with water and ethyl acetate, and extracted twice with ethyl acetate. The combined organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate and filtered, and the solvent was evaporated under reduced pressure. The obtained residue was washed with ethyl acetate to give the title compound (1.5 g, 46%) as a white solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08445509B2 |
| 出典データセット | uspto-grants-2013_05 |
| ORD ID | ord-88bd717f85134423bdc98d0d2c74a780 |
| 出典メモ | uspto-grants-2013_05 |