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HRID 74193作成日:2026年10月25日

Potassium Carbonate → 5-(Benzoxazol-2-yl)-2-(4-pyridyl)-1-(tetrahydropyran-4-yl)benzimidazole

https://huagongshe.com/reaction/74193

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium CarbonateHCID 11430—
反応物4-PyridinecarboxaldehydeHCID 13389—
反応物Potassium hydroxy sulfiteHCID 23707502—
反応物5-(Benzoxazol-2-yl)-2-(tetrahydropyran-4-yl)aminoanilineHCID 67498806—
溶媒WaterHCID 962—
溶媒DimethylformamideHCID 6228—
生成物5-(Benzoxazol-2-yl)-2-(4-pyridyl)-1-(tetrahydropyran-4-yl)benzimidazoleHCID 6749880161%

反応手順

5-(Benzoxazol-2-yl)-2-(tetrahydropyran-4-yl)aminoaniline (see Working Example 20-2) (0.15 g, 0.484 mmol) was dissolved in DMF (3 mL) and water (0.1 mL), 4-pyridinecarboxaldehyde (0.06 g, 0.561 mmol) was added followed by oxone (0.19 g, 0.310 mmol), and this was stirred at room temperature for 2.5 hours. Aqueous potassium carbonate solution (0.09 g/15 mL) was added to the reaction solution. This was extracted with chloroform, washed with water, and after drying over magnesium sulfate, this was concentrated and purified by silica gel column chromatography. The crystals obtained were washed with hexane and a small amount of ethyl acetate, and dried to yield the title compound (117 mg, 60.9% yield) as white crystals.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08829035B2
出典データセットuspto-grants-2014_09
ORD IDord-3f8890607e19440eb5a12f4a4790a777
出典メモuspto-grants-2014_09