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HRID 1877460作成日:2026年10月27日

Hydrogen Peroxide → 4-[4-(6-fluoro-1H-benzimidazol-2-yl)-9H-carbazol-9-yl]-2-(4-hydroxybutan-3(R,S)-ylamino)benzamide

https://huagongshe.com/reaction/1877460

反応式

関与物質

役割名称HCID仕込み量
反応物Hydrogen PeroxideHCID 784—
反応物Potassium CarbonateHCID 11430—
反応物Sodium HydroxideHCID 14798—
反応物2-fluoro-4-[4-(6-fluoro-1H-benzimidazol-2-yl)carbazol-9-yl]benzonitrileHCID 58338358—
溶媒Dimethyl SulfoxideHCID 679—
溶媒EthanolHCID 702—
生成物4-[4-(6-fluoro-1H-benzimidazol-2-yl)-9H-carbazol-9-yl]-2-(4-hydroxybutan-3(R,S)-ylamino)benzamideHCID 68639471—

反応手順

The process is carried out as in stage 3 of Example 3, but using 300 mg of 2-fluoro-4-[4-(6-fluoro-1H-benzimidazol-2-yl)carbazol-9-yl]benzonitrile, obtained according to stage 2 of Example 3, 296 mg of potassium carbonate and 1.273 g of 3(R,S)-aminopropanol in 3 ml of dimethyl sulphoxide. 1.357 ml of a 1M aqueous solution of sodium hydroxide, 1.313 ml of a 30% aqueous solution of hydrogen peroxide and 7 ml of ethanol are then added to the reaction medium. After treatment as in stage 3 of Example 3, then purification by flash chromatography on silica gel, elution being carried out with a mixture of dichloromethane and ethanol (95/5 by volume), followed by crystallization from 10 ml of diisopropyl ether, 165 mg of 4-[4-(6-fluoro-1H-benzimidazol-2-yl)-9H-carbazol-9-yl]-2-(4-hydroxybutan-3(R,S)-ylamino)benzamide are thus obtained in the form of a beige solid, the characteristics of which are the following:

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08309721B2
出典データセットuspto-grants-2012_11
ORD IDord-961315c2db1d40a0b16752e3c8b3d7f5
出典メモuspto-grants-2012_11