1-Bromo-4-fluorobenzene → 1-(4-Fluoro-phenyl)-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-one

関与物質

役割	名称	HCID	仕込み量
反応物	1-Bromo-4-fluorobenzene	HCID 9993	—
反応物	Potassium Carbonate	HCID 11430	—
反応物	1,2-Diaminocyclohexane, trans-	HCID 43806	—
反応物	1-(4-Methylpyridin-3-yl)imidazolidin-2-one	HCID 59636170	—
触媒	Copper iodide	HCID 83717	—
溶媒	1,4-Dioxane	HCID 31275	—
生成物	1-(4-Fluoro-phenyl)-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-one	HCID 59636145	43.5%

反応手順

Using the same reaction conditions as in Example 14, 1-(4-methyl-pyridin-3-yl)-imidazolidin-2-one (I-14b: 150 mg, 0.8465 mmol) was reacted with 1-bromo-4-fluoro-benzene (148.1 mg, 0.8465 mmol), 1,4-dioxane (25 mL), copper iodide (16 mg, 0.08465 mmol), trans-1,2-diamino cyclohexane (29 mg, 0.2539 mmol) and potassium carbonate (468 mg, 3.3860 mmol) to afford the crude product. Purification by column chromatography on silica gel (2% MeOH in chloroform) afforded 100 mg of the product (43% yield).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08263635B2
出典データセット	uspto-grants-2012_09
ORD ID	ord-b0ff1d7550e04b9c84f42ccb41098d30
出典メモ	uspto-grants-2012_09