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HRID 11655作成日:2026年10月23日

Sulfamide → N-[(5-Chloro-2-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-phenyl)-acetyl]-sulfamide

https://huagongshe.com/ja/reaction/11655

反応式

関与物質

役割名称HCID仕込み量
反応物SulfamideHCID 82267—
反応物2-(2-(2-((2R,5S)-4-(4-fluorobenzyl)-2,5-dimethylpiperazin-1-yl)-2-oxoethoxy)-5-chlorophenyl)acetic acidHCID 44431527—
溶媒Thionyl ChlorideHCID 24386—
生成物N-[(5-Chloro-2-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-phenyl)-acetyl]-sulfamideHCID 6965594912.7%

反応手順

A solution of (5-chloro-2-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-phenyl)-acetic acid (0.10 g, 0.21 mmol) in thionyl chloride (2 mL) was stirred at ambient temperature for two hours. The reaction was concentrated to dryness and the crude acid chloride was dissolved in 1,4-dioxane (4 mL) followed by addition of sulfamide (0.022 g, 0.23 mmol). The reaction was stirred at ambient temperature for 3 days. The reaction was concentrated and chromatographed on silica gel to give the title compound (0.014 g, LRMS: 525.1).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07098212B2
出典データセットuspto-grants-2006_08
ORD IDord-735b2820811740bb87abcd492d3e49c9
出典メモuspto-grants-2006_08