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HRID 2190563作成日:2026年10月27日

Diisopropylethylamine → 4-(3-trifluoromethyl-phenyl)-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-5'-carboxylic acid (5-methyl-4-phenyl-thiazol-2-yl)-amide

https://huagongshe.com/reaction/2190563

反応式

関与物質

役割名称HCID仕込み量
反応物DiisopropylethylamineHCID 81531—
反応物6-chloro-N-(5-methyl-4-phenyl-1,3-thiazol-2-yl)pyridine-3-carboxamideHCID 3379941—
反応物4-(3-Trifluoromethylphenyl)piperidine, HClHCID 22252849—
溶媒N-methyl-2-pyrrolidoneHCID 13387—
生成物4-(3-trifluoromethyl-phenyl)-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-5'-carboxylic acid (5-methyl-4-phenyl-thiazol-2-yl)-amideHCID 59317981—

反応条件

温度70 °C

反応手順

To a mixture of 6-chloro-N-(5-methyl-4-phenyl-thiazol-2-yl)-nicotinamide (50 mg, 0.152 mmol) and anhydrous N-methylpyrrolidinone (10 mL) in a sealed tube was added 4-(3-trifluoromethyl-phenyl)-piperidine hydrochloride (80 mg, 0.30 mmol) followed by diisopropylethylamine (0.11 mL, 0.63 mmol). The mixture was heated in an oil bath at 70° C. overnight. After concentration, the crude was purified by RP-HPLC to give 4-(3-trifluoromethyl-phenyl)-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-5′-carboxylic acid (5-methyl-4-phenyl-thiazol-2-yl)-amide as an off-white powder. LCMS calcd for C28H25F3N4OS (m/e) 522, obsd 523 (M+H).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08324385B2
出典データセットuspto-grants-2012_12
ORD IDord-078b12da911f4cd1ac7ec024b44444f8
出典メモuspto-grants-2012_12