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HRID 269563作成日:2026年10月26日

Isobutylamine → Methyl 2''-{[(4-fluorophenyl)methyl]oxy}-5-{[(2-methylpropyl)amino]carbonyl}-5''-(trifluoromethyl)-1,1':2',1''-terphenyl-3-carboxylate

https://huagongshe.com/reaction/269563

反応式

関与物質

役割名称HCID仕込み量
反応物IsobutylamineHCID 6558—
反応物4-MethylmorpholineHCID 7972—
反応物1-Hydroxybenzotriazole hydrateHCID 2796029—
反応物1-(3-Dimethylaminopropyl)ethylcarbodiimide hydrochlorideHCID 21982921—
反応物2''-{[(4-Fluorophenyl)methyl]oxy}-5-[(methyloxy)carbonyl]-5''-(trifluoromethyl)-1,1':2',1''-terphenyl-3-carboxylic acidHCID 58731014—
溶媒DichloromethaneHCID 6344—
溶媒Ethyl AcetateHCID 8857—
生成物Methyl 2''-{[(4-fluorophenyl)methyl]oxy}-5-{[(2-methylpropyl)amino]carbonyl}-5''-(trifluoromethyl)-1,1':2',1''-terphenyl-3-carboxylateHCID 5873101551.8%

反応手順

A mixture of 2″-{[(4-fluorophenyl)methyl]oxy}-5-[(methyloxy)carbonyl]-5″-(trifluoromethyl)-1,1′:2′,1″-terphenyl-3-carboxylic acid (90 mg, 0.17 mmol), 4-methylmorpholine (34 mg, 45 μl, 0.34 mmol), 1-hydroxybenzotriazole hydrate (30 mg, 0.2 mmol), 1-(3-dimethylaminopropyl)-ethylcarbodiimide hydrochloride (38 mg, 0.2 mmol), and isobutylamine (25 mg, 34 ul, 0.34 mmol) in dichloromethane (3 ml) was stirred at room temperature for 2 hours. The mixture was diluted with ethyl acetate (10 ml), then washed with saturated NaHCO3, 2M HCl, water and brine. The organic phase was dried and evaporated. The residue was purified by chromatography in ethyl acetate/hexane (1:9-1:4) to give the title compound as a colourless solid (51 mg, 50%). LCMS: Rt=4.10 min. [M+H] 580

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07446222B2
出典データセットuspto-grants-2008_11
ORD IDord-4047a240d5c644808cfa34e5e1c68e3f
出典メモuspto-grants-2008_11