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Tetrahydrofuran → N-[2-chloro-5-({2-[(cyclopropylcarbonyl)amino][1,2,4]triazolo[1,5-a]pyridin-6-yl}oxy)phenyl]-2-methyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Tetrahydrofuran | HCID 8028 | — |
| 反応物 | Thionyl Chloride | HCID 24386 | — |
| 反応物 | 2-methyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxylic Acid | HCID 2775651 | — |
| 反応物 | N-[6-(3-amino-4-chlorophenoxy)[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide | HCID 57749285 | — |
| 触媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Dimethylacetamide | HCID 31374 | — |
| 生成物 | N-[2-chloro-5-({2-[(cyclopropylcarbonyl)amino][1,2,4]triazolo[1,5-a]pyridin-6-yl}oxy)phenyl]-2-methyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide | HCID 57749379 | 48.1% |
反応手順
In the same manner as in Example 55 and using 2-methyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxylic acid (110 mg, 0.564 mmol), tetrahydrofuran (5 mL), thionyl chloride (97.2 μL, 1.12 mmol), N,N-dimethylformamide (2 drops), N-[6-(3-amino-4-chlorophenoxy)[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide (170 mg, 0.495 mmol) and N,N-dimethylacetamide (6 mL) as starting materials, the title compound (124 mg, 48%) was obtained as a white solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08304557B2 |
| 出典データセット | uspto-grants-2012_11 |
| ORD ID | ord-993ed4cdaa024266a178efdefbb844e3 |
| 出典メモ | uspto-grants-2012_11 |