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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

反応式

関与物質

役割名称HCID仕込み量
反応物4-(Trifluoromethyl)anilineHCID 9964—
反応物p-Toluenesulfonic acid monohydrateHCID 521998—
反応物7-Chloro-2-(2,6-dichlorobenzyl)oxazolo[5,4-d]pyrimidineHCID 57742456—
溶媒TolueneHCID 1140—
生成物[2-(2,6-Dichloro-benzyl)-oxazolo[5,4-d]pyrimidin-7-yl]-(4-trifluoromethyl-phenyl)-amineHCID 4264213535%

反応条件

温度120 °C

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

DOI10.6084/m9.figshare.5104873.v1
特許番号US08637527B2
出典データセットuspto-grants-2014_01
ORD IDord-10a77e24097045c0930697f016229ca9
出典メモuspto-grants-2014_01