戻る
化工社化工社 化学情報印刷レポート · 研究参考用
HRID 547079作成日:2026年10月26日

1-Ethynylcyclohexanol → [5-(4-{1-ethyl-1-[4-(1-hydroxy-cyclohexylethynyl)-3-methyl-phenyl]-propyl}-phenyl)-pyridin-3-yl]-acetic Acid Methyl Ester

https://huagongshe.com/reaction/547079

反応式

関与物質

役割名称HCID仕込み量
反応物1-EthynylcyclohexanolHCID 6525—
反応物TriethylamineHCID 8471—
反応物(5-{4-[1-Ethyl-1-(3-methyl-4-trifluoromethanesulfonyloxy-phenyl)-propyl]-phenyl}-pyridin-3-yl)-acetic acid methyl esterHCID 57709113—
触媒Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI)HCID 24350—
溶媒AcetonitrileHCID 6342—
生成物[5-(4-{1-ethyl-1-[4-(1-hydroxy-cyclohexylethynyl)-3-methyl-phenyl]-propyl}-phenyl)-pyridin-3-yl]-acetic Acid Methyl EsterHCID 5770902867.1%

反応条件

温度160 °C

反応手順

Triethylamine (0.156 mL, 1.12 mmol), tetrakistriphenylphosphine palladium (43.0 mg, 0.036 mmol) and copper (I) iodide (7.0 mg, 0.037 mmol) were added to a solution of (5-{4-[1-ethyl-1-(3-methyl-4-trifluoromethanesulfonyloxy-phenyl)-propyl]-phenyl}-pyridin-3-yl)-acetic acid methyl ester (Example 144-(2); 0.1 g, 0.186 mmol) and 1-ethynyl-cyclohexanol (69.6 mg, 0.56 mmol) in acetonitrile (0.9 mL), and the mixture was stirred with microwave heating at 160° C. for five minutes. The reaction solution was purified by silica gel chromatography (hexane:ethyl acetate=1:1) to give the title compound (63.6 mg, 66%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07935688B2
出典データセットuspto-grants-2011_05
ORD IDord-89482fde943340a5ae50deb3e05b0669
出典メモuspto-grants-2011_05