4-(Trifluoromethyl)aniline → [2-(2,6-Dichloro-benzyl)-oxazolo[5,4-d]pyrimidin-7-yl]-(4-trifluoromethyl-phenyl)-amine

https://huagongshe.com/ko/reaction/474306

참여 물질

역할	이름	HCID	투입량
반응물	4-(Trifluoromethyl)aniline	HCID 9964	—
반응물	p-Toluenesulfonic acid monohydrate	HCID 521998	—
반응물	7-Chloro-2-(2,6-dichlorobenzyl)oxazolo[5,4-d]pyrimidine	HCID 57742456	—
용매	Toluene	HCID 1140	—
생성물	[2-(2,6-Dichloro-benzyl)-oxazolo[5,4-d]pyrimidin-7-yl]-(4-trifluoromethyl-phenyl)-amine	HCID 42642135	35%

반응 조건

온도	120 °C

반응 단계

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).

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US08637527B2
출처 데이터셋	uspto-grants-2014_01
ORD ID	ord-10a77e24097045c0930697f016229ca9
출처 메모	uspto-grants-2014_01