Potassium Phosphate, Tribasic → 1-(Benzo[b]thiophen-5-yl)-3-(4-cyclopropylpyridin-3-yl)imidazolidin-2-one

関与物質

役割	名称	HCID	仕込み量
反応物	Potassium Phosphate, Tribasic	HCID 62657	—
反応物	trans-N,N'-dimethyl-1,2-cyclohexanediamine	HCID 2733821	—
反応物	5-Bromo-1-benzothiophene	HCID 2776578	—
反応物	1-(4-Cyclopropylpyridin-3-yl)imidazolidin-2-one	HCID 70982007	—
触媒	Copper iodide	HCID 83717	—
生成物	1-(Benzo[b]thiophen-5-yl)-3-(4-cyclopropylpyridin-3-yl)imidazolidin-2-one	HCID 66576484	13%

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: 70 mg, 0.344 mmol) was reacted with 5-bromobenzo[b]thiophene (88.1 mg, 0.413 mmol) 1,4-dioxane (5 mL), copper iodide (6.5 mg, 0.034 mmol), trans-N,N′-dimethylcyclohexane-1,2-diamine (4.8 mg, 0.034 mmol) and potassium phosphate (219 mg, 1.034 mmol) to afford the crude product. Purification by preparative HPLC afforded 15 mg of the product (13% 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-127d44b311584c0091f99dbe43c11676
出典メモ	uspto-grants-2016_05