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HRID 80090作成日:2026年10月23日

1,2-Diaminocyclohexane, trans- → 1-(2,2-Difluoro-benzo[1,3]dioxol-5-yl)-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-one

https://huagongshe.com/ja/reaction/80090

反応式

関与物質

役割名称HCID仕込み量
反応物1,2-Diaminocyclohexane, trans-HCID 43806—
反応物Potassium Phosphate, TribasicHCID 62657—
反応物5-Bromo-2,2-difluoro-1,3-benzodioxoleHCID 2736271—
反応物1-(4-Methylpyridin-3-yl)imidazolidin-2-oneHCID 59636170—
触媒Copper iodideHCID 83717—
溶媒1,4-DioxaneHCID 31275—
生成物1-(2,2-Difluoro-benzo[1,3]dioxol-5-yl)-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-oneHCID 4987214892.2%

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, 0.84650 mmol) was reacted with 5-bromo-2,2-difluoro-benzo[1,3]dioxole (200.6 mg, 0.84650 mmol), 1,4-dioxane (50 mL), copper iodide (16 mg, 0.084650 mmol), trans-1,2-diamino cyclohexane (29 mg, 0.2539 mmol) and potassium phosphate (538 mg, 2.539 mmol) to afford the crude product. Purification by column chromatography on silica gel (2% MeOH in DCM) afforded 260 mg of the product (92% yield).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号USRE045173E1
出典データセットuspto-grants-2014_09
ORD IDord-a13c01077c164d728795c5fbebbd9ddc
出典メモuspto-grants-2014_09