Benzene, 1-bromo-3-(trifluoromethyl)- → 1-(4-Cyclopropylpyridin-3-yl)-3-(3-(trifluoromethyl) phenyl)imidazolidin-2-one

関与物質

役割	名称	HCID	仕込み量
反応物	Benzene, 1-bromo-3-(trifluoromethyl)-	HCID 9817	—
反応物	Potassium Phosphate, Tribasic	HCID 62657	—
反応物	trans-N,N'-dimethyl-1,2-cyclohexanediamine	HCID 2733821	—
反応物	1-(4-Cyclopropylpyridin-3-yl)imidazolidin-2-one	HCID 70982007	—
触媒	Copper iodide	HCID 83717	—
溶媒	1,4-Dioxane	HCID 31275	—
生成物	1-(4-Cyclopropylpyridin-3-yl)-3-(3-(trifluoromethyl) phenyl)imidazolidin-2-one	HCID 66576485	80%

反応手順

Using analogous reagents and reaction conditions as described in Example 1 above, 1-(4-cyclopropylpyridin-3-yl)imidazolidin-2-one (I-1d: 150 mg, 0.738 mmol) was reacted with 1-bromo-3-(trifluoromethyl)benzene (831 mg, 3.69 mmol), 1,4-dioxane (10 mL), copper iodide (14.0 mg, 0.073 mmol), trans-N,N′-dimethylcyclohexane-1,2-diamine (8.4 mg, 0.073 mmol) and potassium phosphate (469.9 mg, 2.21 mmol) to afford the crude product. Purification by column chromatography on silica gel (1.5% methanol in CHCl3) afforded 205 mg of the product (80% yield).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US09339501B2
出典データセット	uspto-grants-2016_05
ORD ID	ord-f5167e4067e04c5c90cbeb8a8019c711
出典メモ	uspto-grants-2016_05