7-Chloro-benzo[1,4]dioxin-2-one → 2-(4-Chloro-2-hydroxy-phenoxy)-1-[4-(4-fluoro-benzyl)-(2R)-2-methyl-piperazin-1-yl]-ethanone

関与物質

役割	名称	HCID	仕込み量
反応物	7-Chloro-benzo[1,4]dioxin-2-one	HCID 3255318	—
反応物	(r)-1-(4-Fluorobenzyl)-3-methylpiperazine	HCID 11600914	—
溶媒	Toluene	HCID 1140	—
生成物	2-(4-Chloro-2-hydroxy-phenoxy)-1-[4-(4-fluoro-benzyl)-(2R)-2-methyl-piperazin-1-yl]-ethanone	HCID 69655856	52.9%

反応条件

温度	95 °C

反応手順

To a solution of 7-chloro-benzo[1,4]dioxin-2-one (0.845 g, 4.81 mmol) in toluene (25 mL) was added (3R)-1-(4-fluoro-benzyl)-3-methyl-piperazine (1.003 g, 4.81 mmol). The resulting mixture was heated to 95° C. overnight. The reaction was cooled to ambient temperature, filtered and concentrated in vacuo. Chromatography on silica gel gave the title compound (˜1 g).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US07098212B2
出典データセット	uspto-grants-2006_08
ORD ID	ord-6326dfff423e40298d12cdfe41a6ac19
出典メモ	uspto-grants-2006_08