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HRID 1744592作成日:2026年10月25日

Potassium Carbonate → N-{3-Cyano-4-[4-(2-hydroxyethyl)piperazin-1-yl]phenyl}-1-(4-fluorophenyl)pyrrole-2-carboxamide

https://huagongshe.com/reaction/1744592

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium CarbonateHCID 11430—
反応物1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimideHCID 15908—
反応物1-HydroxybenzotriazoleHCID 75771—
反応物1-(4-fluorophenyl)-1H-pyrrole-2-carboxylic acidHCID 17390044—
反応物5-Amino-2-[4-(2-hydroxyethyl)piperazin-1-yl]benzonitrileHCID 17609593—
溶媒DimethylformamideHCID 6228—
生成物N-{3-Cyano-4-[4-(2-hydroxyethyl)piperazin-1-yl]phenyl}-1-(4-fluorophenyl)pyrrole-2-carboxamideHCID 2222819535.5%

反応手順

1-(4-Fluorophenyl)pyrrole-2-carboxylic acid (2 g), 5-amino-2-[4-(2-hydroxyethyl)piperazin-1-yl]benzonitrile (2.4 g), 1-hydroxybenzotriazole (1.8 g) and 1-ethyl-3-(3′-dimethylaminopropyl)carbodiimide (2.2 g) were added to dimethylformamide (25 ml) and the mixture was stirred at room temperature for 5 h. The reaction mixture was treated with aqueous potassium carbonate solution and extracted with ethyl acetate. The organic layer was washed with saturated brine and dried over anhydrous magnesium sulfate, after which the solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography (mobile phase:chloroform:methanol=100:1) to give an oily substance. The obtained oily substance was recrystallized from a mixed solvent of toluene-n-hexane to give the title compound (1.5 g), melting point: 170–171° C.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07015218B1
出典データセットuspto-grants-2006_03
ORD IDord-390c5e2179a641e698966627071479d8
出典メモuspto-grants-2006_03