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HRID 499825作成日:2026年10月27日

8-Hydroxyquinoline → 5-chloro-N-((1-(4-(3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)phenyl)-1H-imidazol-4-yl)methyl)thiophene-2-carboxamide

https://huagongshe.com/reaction/499825

反応式

関与物質

役割名称HCID仕込み量
反応物8-HydroxyquinolineHCID 1923—
反応物Potassium CarbonateHCID 11430—
反応物3-MethyluracilHCID 79066—
反応物5-Chloro-N-((1-(4-iodophenyl)-1H-imidazol-4-yl)methyl)thiophene-2-carboxamideHCID 24986897—
触媒Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI)HCID 24350—
溶媒Dimethyl SulfoxideHCID 679—
生成物5-chloro-N-((1-(4-(3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)phenyl)-1H-imidazol-4-yl)methyl)thiophene-2-carboxamideHCID 2476016122.6%

反応条件

温度130 °C

反応手順

A mixture of 5-chloro-N-((1-(4-iodophenyl)-1H-imidazol-4-yl)methyl)thiophene-2-carboxamide 1-6 (66 mg, 0.15 mmol), 3-methyluracil (60 mg, 0.48 mmol), 8-hydroxyquinoline (10 mg, 0.069 mmol) and K2CO3 (60 mg, 0.43 mmol) in DMSO (1 mL) was degassed with Ar before being charged with CuI (15 mg, 0.079 mmol). The mixture in a sealed tube was heated at 130° C. overnight. The mixture was then purified by HPLC to give the titled compound (15 mg). MS 442.2 and 444.2 (M+H, Cl pattern).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07767697B2
出典データセットuspto-grants-2010_08
ORD IDord-a16ae4c725d3430f80908d23c4bca53d
出典メモuspto-grants-2010_08