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HRID 474306作成日:2026年10月24日
4-(Trifluoromethyl)aniline → [2-(2,6-Dichloro-benzyl)-oxazolo[5,4-d]pyrimidin-7-yl]-(4-trifluoromethyl-phenyl)-amine
https://huagongshe.com/ja/reaction/474306
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 4-(Trifluoromethyl)aniline | HCID 9964 | — |
| 反応物 | p-Toluenesulfonic acid monohydrate | HCID 521998 | — |
| 反応物 | 7-Chloro-2-(2,6-dichlorobenzyl)oxazolo[5,4-d]pyrimidine | HCID 57742456 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 生成物 | [2-(2,6-Dichloro-benzyl)-oxazolo[5,4-d]pyrimidin-7-yl]-(4-trifluoromethyl-phenyl)-amine | HCID 42642135 | 35% |
反応手順
A mixture of 7-chloro-2-(2,6-dichloro-benzyl)-oxazolo[5,4-d]pyrimidine (42 mg, 0.13 mmol), 4-trifluoromethyl-phenylamine (22 mg, 0.13 mmol), and p-TsOH.H2O (51 mg, 0.27 mmol) in toluene (2 mL) was heated to 120° C. in a sealed tube. After 2 h, the solution was cooled purified by preparative reverse-phase HPLC to afford the title compound as a colorless solid (20 mg, 34%). MS (ESI): mass calcd. C19H11Cl2F3N4O, 438.0; m/z found, 439.1 [M+H]+. 1H NMR (CDCl3): 8.57 (s, 1H), 7.90 (d, J=8.6 Hz, 2H), 7.76 (s, 1H), 7.62 (d, J=8.6 Hz, 2H), 7.42 (d, J=8.0 Hz, 2H), 7.31-7.27 (m, 1H), 4.66 (s, 2H).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08637527B2 |
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| 出典データセット | uspto-grants-2014_01 |
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| ORD ID | ord-10a77e24097045c0930697f016229ca9 |
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| 出典メモ | uspto-grants-2014_01 |
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