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HRID 507208作成日:2026年10月26日

Benzoyl chloride → [4-[6-Fluoro-2-phenoxymethyl-3-(4-trifluoromethoxy-benzyl)-3H-benzoimidazol-5-yl]-piperazin-1-yl}-phenyl-methanone

https://huagongshe.com/reaction/507208

反応式

関与物質

役割名称HCID仕込み量
反応物Benzoyl chlorideHCID 7412—
反応物5-fluoro-2-phenoxymethyl-6-piperazin-1-yl-1-(4-trifluoromethoxy-benzyl)-1H-benzoimidazoleHCID 68467102—
溶媒DichloromethaneHCID 6344—
生成物[4-[6-Fluoro-2-phenoxymethyl-3-(4-trifluoromethoxy-benzyl)-3H-benzoimidazol-5-yl]-piperazin-1-yl}-phenyl-methanoneHCID 1163576073.4%

反応手順

80 mg of 5-fluoro-2-phenoxymethyl-6-piperazin-1-yl-1-(4-trifluoromethoxy-benzyl)-1H-benzoimidazole (0.16 mmol) and 0.033 ml TEA (0.24 mmol) were dissolved in 1.5 ml dichloromethane and treated with 0.023 ml benzoylchloride (0.2 mmol). After 4 h of stirring at rt, the reaction mixture was diluted with dichloromethane, washed with water, saturated sodium bicarbonate and brine, dried with magnesium sulfate, filtered and concentrated in vacuo, leading to 85 mg yellow solid which was purified by column chromatography (10 g silicagel, dichloromethane/methanol 30:1). 71 mg product as a light yellow solid (73%) was obtained. MS (ISP) 605.3 (M+H)+.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07786128B2
出典データセットuspto-grants-2010_08
ORD IDord-01c27ff5e6d24eb883f49ecfaefe5106
出典メモuspto-grants-2010_08