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HRID 131228作成日:2026年10月27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/131228

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US07384945B2
出典データセットuspto-grants-2008_06
ORD IDord-afc4d145a5e5426895eb8cae854a74c4
出典メモuspto-grants-2008_06