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HRID 336178作成日:2026年10月24日

Hydrochloric Acid → 3'-Chloro-5'-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-3-carboxylic acid (5-tert-butyl-isoxazol-3-yl)-amide

https://huagongshe.com/ja/reaction/336178

反応式

関与物質

役割名称HCID仕込み量
反応物Hydrochloric AcidHCID 313—
反応物TriethylamineHCID 8471—
反応物3-Chloro-2-fluoro-5-(trifluoromethyl)pyridineHCID 1268075—
反応物HCID 58563805HCID 58563805—
溶媒tert-ButanolHCID 6386—
生成物3'-Chloro-5'-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-3-carboxylic acid (5-tert-butyl-isoxazol-3-yl)-amideHCID 46872043—

反応条件

温度175 °C

反応手順

A microwave reaction vial is charged with piperidine-3-carboxylic acid (5-tert-butyl-isoxazol-3-yl)-amide; hydrochloride (94 mg; 0.327 mmol), 3-chloro-2-fluoro-5-trifluoromethylpyridine (0.043 mL; 0.33 mmol), triethylamine (0.092 mL; 0.66 mmol) and t-butanol (0.5 mL). The vial is heated in microwave at 175° C. for 1 hour then left standing at room temperature overnight. The reaction mixture is concentrated in vacuo. Purification by flash chromatography on silica using methanol/methylene chloride then recrystallization from hot methanol provides the title compound, m/z 431 [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-b7d621c0d7a44d1389355d608ad1b156
出典メモuspto-grants-2014_11