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HRID 1513221作成日:2026年10月25日

Morpholine → 2-(2,6-Dimethyl-4-morpholin-4-yl-phenyl)-3H-benzoimidazole-5-carboxylic acid methyl ester

https://huagongshe.com/reaction/1513221

反応式

関与物質

役割名称HCID仕込み量
反応物MorpholineHCID 8083—
反応物Potassium Phosphate, TribasicHCID 62657—
反応物2-(2,6-Dimethyl-4-trifluoromethanesulfonyloxy-phenyl)-3H-benzoimidazole-5-carboxylic acid methyl esterHCID 86632816—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒WaterHCID 962—
溶媒TolueneHCID 1140—
溶媒HeptaneHCID 8900—
生成物2-(2,6-Dimethyl-4-morpholin-4-yl-phenyl)-3H-benzoimidazole-5-carboxylic acid methyl esterHCID 66966397—

反応条件

温度80 °C

反応手順

To a stirred solution of 2.4 g of 2-(2,6-Dimethyl-4-trifluoromethanesulfonyloxy-phenyl)-3H-benzoimidazole-5-carboxylic acid methyl ester in 6 ml of toluene was added 4 ml of morpholine, 280 mg of Pd2(dba)3, 400 mg of P(biphenyl)t -Bu2 and 2.0 g of K3PO4. The reaction vessel sealed and heated at 80° C. overnight. The reaction was cooled to room temperature and diluted with water and heptane. The resulting precipitates were collected by filtration, washed with water and dried to afford the title compound. LCMS retention T=1.14 min, m/z=366.2, Method 10.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08217065B2
出典データセットuspto-grants-2012_07
ORD IDord-f028f19ac43b4fe192fb6ae8f3a09cce
出典メモuspto-grants-2012_07