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HRID 19495作成日:2026年10月24日

4,6-Dichloropyrimidine → N-{3-[1-(6-chloro-pyrimidin-4-yl)-1H-imidazol-2-ylamino]-4-methyl-phenyl}-3-trifluoromethyl-benzamide

https://huagongshe.com/ja/reaction/19495

反応式

関与物質

役割名称HCID仕込み量
反応物4,6-DichloropyrimidineHCID 70943—
反応物DiisopropylethylamineHCID 81531—
反応物N-[3-(1H-Imidazol-2-ylamino)-4-methyl-phenyl]-3-trifluoromethyl-benzamideHCID 58973096—
溶媒(+-)-2-ButanolHCID 6568—
生成物N-{3-[1-(6-chloro-pyrimidin-4-yl)-1H-imidazol-2-ylamino]-4-methyl-phenyl}-3-trifluoromethyl-benzamideHCID 58973058—

反応条件

温度110 °C

反応手順

A mixture of N-[3-(1H-Imidazol-2-ylamino)-4-methyl-phenyl]-3-trifluoromethyl-benzamide (330 mg, 0.92 mmol), 4,6-dichloropyrimidine (409 mg, 2.75 mmol), N,N-diisopropylethyl amine (500 μL, 2.87 mmol) in 2-butanol (20 mL) is heated at 110° C. After 16 hours, the reaction mixture is concentrated. The solid is washed with saturated sodium carbonate, water, ethyl acetate, and dried to give the title compound. 1H NMR 600 MHz (DMSO-d6) δ 10.71 (s, 1H), 10.50 (s, 1H), 9.09 (s, 1H), 8.80 (s, 1H), 8.33 (s, 1H), 8.29 (d, J=7.8 Hz, 1H), 8.17 (s, 1H), 7.96 (d, J=8.4 Hz, 1H), 7.84 (s, 1H), 7.77 (t, J=8.4 Hz, 1H), 7.42 (d, J=7.2 Hz, 1H), 7.21 (d, J=8.4 Hz, 1H), 6.95 (s, 1H), 2.38 (s, 3H); MS m/z 473.3 (M+1).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07745437B2
出典データセットuspto-grants-2010_06
ORD IDord-ca0b4baae053415c9b2d4bcefe18a839
出典メモuspto-grants-2010_06