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HRID 1667758作成日:2026年10月25日

Dimethylformamide → 4-(3-Chloro-phenyl)-2-{6-[2-hydroxy-3-(4-methyl-piperazin-1-yl)-propoxy]-benzoimidazol-1-yl}-thiazole-5-carboxylic acid amide

https://huagongshe.com/reaction/1667758

反応式

関与物質

役割名称HCID仕込み量
反応物DimethylformamideHCID 6228—
反応物MorpholineHCID 8083—
反応物Potassium CarbonateHCID 11430—
反応物4-(3-Chloro-phenyl)-2-(6-oxiranylmethoxy-benzoimidazol-1-yl)-thiazole-5-carboxylic acid amideHCID 86642834—
生成物4-(3-Chloro-phenyl)-2-{6-[2-hydroxy-3-(4-methyl-piperazin-1-yl)-propoxy]-benzoimidazol-1-yl}-thiazole-5-carboxylic acid amideHCID 46832304—

反応手順

A mixture of 0.021 g (0.05 mmole) of 4-(3-chloro-phenyl)-2-(6-oxiranylmethoxy-benzoimidazol-1-yl)-thiazole-5-carboxylic acid amide (I.39a), 0.5 mL of dimethylformamide, 0.035 g (0.25 mmole) of potassium carbonate and 0.009 mL (0.1 mmole) of morpholine was heated at 100 degrees for 3 hours. The mixture was cooled, the solid was removed by filtration and the filtrate purified by reverse phase silica gel chromatography, eluting with acetonitrile-water (gradient 20:80-100:0) to give 0.012 g of 4-(3-chloro-phenyl)-2-{6-[2-hydroxy-3-(4-methyl-piperazin-1-yl)-propoxy]-benzoimidazol-1-yl}-thiazole-5-carboxylic acid amide (I.40) as a white powder. MH+/Z=514

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08044213B2
出典データセットuspto-grants-2011_10
ORD IDord-08b1d3d4c5244cdabc16e8643091fcd1
出典メモuspto-grants-2011_10