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HRID 80225作成日:2026年10月23日

1,2-Diaminocyclohexane → 1-Benzothiazol-6-yl-3-pyridin-3-yl-4-trifluoromethyl-imidazolidin-2-one

https://huagongshe.com/ja/reaction/80225

反応式

関与物質

役割名称HCID仕込み量
反応物1,2-DiaminocyclohexaneHCID 4610—
反応物3-BromopyridineHCID 12286—
反応物Potassium Phosphate, TribasicHCID 62657—
反応物1-Benzothiazol-6-yl-4-trifluoromethyl-imidazolidin-2-oneHCID 68787913—
触媒Copper iodideHCID 83717—
溶媒1,4-DioxaneHCID 31275—
生成物1-Benzothiazol-6-yl-3-pyridin-3-yl-4-trifluoromethyl-imidazolidin-2-oneHCID 4987264923.8%

反応手順

Using the same reaction conditions and work up as described in example 1, step-3,1-Benzothiazol-6-yl-4-trifluoromethyl-imidazolidin-2-one (I-170b: 50 mg, 0.174 mmol) was refluxed with 3-Bromo-pyridine (33 mg, 0.209 mmol), copper iodide (3.3 mg, 0.0174 mmol), Cyclohexane-1,2-diamine (6 mg, 0.0522 mmol), potassium phosphate (110 mg, 0.522 mmol) and 1,4-Dioxane (2 mL) at 120° C. for 12 hours to afford the crude product. Purification by column chromatography on silica gel (2% methanol in chloroform) followed by n-pentane washing afforded 15 mg of the product (23.8% 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-10082d1ae133471d889e5801d44f73b2
出典メモuspto-grants-2014_09