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

참여 물질

역할	이름	HCID	투입량
반응물	Pyridine	HCID 1049	—
반응물	Phosphorus oxychloride	HCID 24813	—
반응물	3-Tert-butyl-1,2-oxazol-5-amine	HCID 2095694	—
반응물	(S)-1-(4-Chloro-phenyl)-6-oxo-piperidine-2-carboxylic acid	HCID 42127104	—
용매	Water	HCID 962	—
생성물	(S)-1-(4-Chloro-phenyl)-6-oxo-piperidine-2-carboxylic acid (3-tert-butyl-isoxazol-5-yl)-amide	HCID 58563752	—

반응 조건

온도	0 °C

반응 단계

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+].

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US08889670B2
출처 데이터셋	uspto-grants-2014_11
ORD ID	ord-cc60fa4f3eba4880b745e202d0cd6112
출처 메모	uspto-grants-2014_11