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HRID 1358754作成日:2026年10月26日

Triethylamine → N-(2-Ethylamino-5-trifluoromethanesulfonyl-phenyl)-2-(4-methanesulfonyl-phenyl)-acetamide

https://huagongshe.com/reaction/1358754

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物1-HydroxybenzotriazoleHCID 75771—
反応物4-Mesylphenylacetic acidHCID 572345—
反応物N1-ethyl-4-trifluoromethanesulfonylbenzene-1,2-diamineHCID 703518—
溶媒AcetonitrileHCID 6342—
生成物N-(2-Ethylamino-5-trifluoromethanesulfonyl-phenyl)-2-(4-methanesulfonyl-phenyl)-acetamideHCID 9956080—

反応手順

To a solution of 4-methylsulfonylphenylacetic acid (100 mg, 0.467 mmol) in acetonitrile was added 1-hydroxybenzotriazole (76 mg, 0.56 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carboiimide hydrochloride (108 mg, 0.56 mmol), triethylamine (0.143 mL, 1.03 mmol) and N1-ethyl-4-[(trifluoromethyl)sulfonyl]benzene-1,2-diamine (125 mg, 0.467 mmol). The mixture was stirred at room temperature for overnight. The reaction was extracted with ethyl acetate, washed with water and brine, dried, concentrated and recrystallized from ethyl acetate to give the title compound. 1H NMR (300 MHz, DMSO-d6) δ9.54 (br s, 1H, NH), 7.88 (d, J=8.3 Hz, 2H), 7.75 (d, J=2.1 Hz, 1H), 7.64 (dd, 1H), 7.61 (d, J=8.3 Hz, 2H), 6.90 (d, J=9.0 Hz, 1H), 6.70 (t, J=5.2 Hz, 1H, NH), 3.86 (s, 2H, CH2), 3.31 (s, 3H, CH3), 3.29 (m, 2H, NCH2CH3), 1.20 (t, J=7.1 Hz, 3H, NCH2CH3). MS 465 [M++1].

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06596772B1
出典データセットuspto-grants-2003_07
ORD IDord-ba4f8aed8a1b4c888778176ca726eb1f
出典メモuspto-grants-2003_07