Hydrochloric Acid → (S)-3'-Chloro-5'-trifluoromethyl-3,4,5,6-tetrahydro-2H-1,2'-bipyridinyl-2-carboxylic acid (3-phenyl-1,2,4-thiadiazol-5-yl)-amide

関与物質

役割	名称	HCID	仕込み量
反応物	Hydrochloric Acid	HCID 313	—
反応物	Diisopropylethylamine	HCID 81531	—
反応物	3-Chloro-2-fluoro-5-(trifluoromethyl)pyridine	HCID 1268075	—
反応物	(S)-Piperidine-2-carboxylic acid (3-phenyl-1,2,4-thiadiazol-5-yl)-amide	HCID 70865032	—
溶媒	Dimethyl Sulfoxide	HCID 679	—
生成物	(S)-3'-Chloro-5'-trifluoromethyl-3,4,5,6-tetrahydro-2H-1,2'-bipyridinyl-2-carboxylic acid (3-phenyl-1,2,4-thiadiazol-5-yl)-amide	HCID 46872494	—

反応条件

温度	100 °C

反応手順

To a stirred solution of (S)-Piperidine-2-carboxylic acid (3-phenyl-1,2,4-thiadiazol-5-yl)-amide; hydrochloride (70 mg; 0.215 mmol) and N,N-diisopropylethylamine (0.037 mL; 0.215 mmol) in DMSO (1 mL) is added 3-chloro-2-fluoro-5-trifluoromethylpyridine (42.9 mg; 0.215 mmol). The reaction mixture is heated at 100° C. for 4 hours. Purification by flash chromatography on silica gel using methanol/methylene chloride provides the title compound, m/z 468 [M+H+].

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08889670B2
出典データセット	uspto-grants-2014_11
ORD ID	ord-48562b6b8db94cf8bdb9f1d8ed68eb33
出典メモ	uspto-grants-2014_11