関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 1-(Azidomethyl)-3,5-bis(trifluoromethyl)benzene | HCID 44185743 | — |
| 反応物 | (2-Chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone | HCID 136347867 | — |
| 溶媒 | Isopropanol | HCID 3776 | — |
| 生成物 | Tradipitant | HCID 9916461 | — |
反応手順
The reaction can also be carried out using (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone (30.0 g; 72.3 mmol; 1.0 equiv) in isopropanol (225 mL). 1-azidomethyl-3,5-bistrifluoromethylbenzene (20.43 g; 76 mmol; 1.05 equiv) and potassium carbonate (5.0 g; 36.2 mmol; 0.5 equiv) are added, and the reaction mixture is heated to reflux for 21-24 hours. Cool the reaction mixture to 20° C., add water (120 mL), and stir for approximately 16 hours. Filter, wash with 120 mL isopropanol/water (1:1 v/v), and dry under reduced pressure at 50° C. to yield the title compound, which may be recrystallized as described above.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07381826B2 |
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| 出典データセット | uspto-grants-2008_06 |
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| ORD ID | ord-4783d67d115340ea998b33d74f29b382 |
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| 出典メモ | uspto-grants-2008_06 |
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