1-Butanol, 4-methoxy- → 2-(3,5-Bis-(4-fluoro-phenyl)-(1,2,4)triazol-1-yl]-1-(4-(6-(4-methoxy-butoxy)-pyrimidin-4-yl)-piperazin-1-yl)-ethanone

関与物質

役割	名称	HCID	仕込み量
反応物	1-Butanol, 4-methoxy-	HCID 8107	—
反応物	Potassium Carbonate	HCID 11430	—
反応物	2-(3,5-Bis-(4-fluoro-phenyl)-(1,2,4)triazol-1-yl)-1-(4-(6-chloro-pyrimidin-4-yl)-piperazin-1-yl)-ethanone	HCID 86690173	—
溶媒	N-methyl-2-pyrrolidone	HCID 13387	—
生成物	2-(3,5-Bis-(4-fluoro-phenyl)-(1,2,4)triazol-1-yl]-1-(4-(6-(4-methoxy-butoxy)-pyrimidin-4-yl)-piperazin-1-yl)-ethanone	HCID 86690176	51%

反応条件

温度	200 °C

反応手順

50 mg 2-(3,5-Bis-(4-fluoro-phenyl)-(1,2,4)triazol-1-yl)-1-(4-(6-chloro-pyrimidin-4-yl)-piperazin-1-yl)-ethanone and 53 mg 4-methoxy-1-butanol were added to 14 mg potassiumcarbonate in 2 mL n-methyl-2-pyrrolidinone. The reaction was sonicated for a few minutes and stirred 30 min at 200° C. The reaction was purified by HPLC to give 29 mg desired product. Rt: 1.82 min (method N), (M+H)+: 564

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08889677B2
出典データセット	uspto-grants-2014_11
ORD ID	ord-402a91ef6b1045cebc0f7d5f64359313
出典メモ	uspto-grants-2014_11