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HRID 18511作成日:2026年10月26日

Bis(2-oxo-3-oxazolidinyl)phosphinic chloride → 1H-Benzoimidazole-2-carboxylic acid (1-pyrimidin-4-yl-piperidin-4-yl)-amide

https://huagongshe.com/reaction/18511

反応式

関与物質

役割名称HCID仕込み量
反応物Bis(2-oxo-3-oxazolidinyl)phosphinic chlorideHCID 152842—
反応物2-Benzimidazolecarboxylic acidHCID 233240—
反応物Sodium BicarbonateHCID 516892—
反応物1-Pyrimidin-4-yl-piperidin-4-ylamine trifluoroacetateHCID 22394384—
溶媒DimethylformamideHCID 6228—
溶媒TriethylamineHCID 8471—
生成物1H-Benzoimidazole-2-carboxylic acid (1-pyrimidin-4-yl-piperidin-4-yl)-amideHCID 86009867—

反応手順

To a solution of 80 mg 1H-Benzoimidazole-2-carboxylic acid in 1 mL DMF and 0.2 mL NEt3, 200 mg 1-Pyrimidin-4-yl-piperidin-4-ylamine trifluoroacetate and 125 mg BOP-Cl were added and the mixture was stirred for 3 h. Finally, 3 mL saturated NaHCO3 solution were added and the mixture was filtered through a chem elut® cartridge by elution with ethyl acetate. After removal of the solvent under reduced pressure the crude product was subjected to the next reaction step without further purification. Yield: 160 mg.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07741341B2
出典データセットuspto-grants-2010_06
ORD IDord-79f71b05143e49688872fd3f6a5d773c
出典メモuspto-grants-2010_06