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HRID 336200作成日:2026年10月26日

Pyridine → (S)-1-(4-Chloro-phenyl)-6-oxo-piperidine-2-carboxylic acid (3-tert-butyl-isoxazol-5-yl)-amide

https://huagongshe.com/reaction/336200

反応式

関与物質

役割名称HCID仕込み量
反応物PyridineHCID 1049—
反応物Phosphorus oxychlorideHCID 24813—
反応物3-Tert-butyl-1,2-oxazol-5-amineHCID 2095694—
反応物(S)-1-(4-Chloro-phenyl)-6-oxo-piperidine-2-carboxylic acidHCID 42127104—
溶媒WaterHCID 962—
生成物(S)-1-(4-Chloro-phenyl)-6-oxo-piperidine-2-carboxylic acid (3-tert-butyl-isoxazol-5-yl)-amideHCID 58563752—

反応条件

温度0 °C

反応手順

To a cold slurry of (S)-1-(4-Chloro-phenyl)-6-oxo-piperidine-2-carboxylic acid (0.2 g; 0.788 mmol) and 5-amino-3-tert-butylisoxazole (0.110 g; 0.788 mmol) in pyridine (0.956 mL; 11.820 mmol) is added phosphorous oxychloride (0.088 mL; 0.946 mmol). The mixture is stirred at 0° C. for 30 minutes and then diluted with water and extracted with ethyl acetate several times. The organics are combined and washed with water and brine, dried (Na2SO4), filtered and concentrated in vacuo. Purification by preparative HPLC affords title compound, m/z 376 [M+H+].

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08889670B2
出典データセットuspto-grants-2014_11
ORD IDord-cc60fa4f3eba4880b745e202d0cd6112
出典メモuspto-grants-2014_11