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HRID 559800作成日:2026年10月26日

Butyl vinyl ether → 5-(1-Butoxyvinyl)-6-methyl-N-[4-(methylsulfonyl)benzyl]-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide

https://huagongshe.com/reaction/559800

反応式

関与物質

役割名称HCID仕込み量
反応物Butyl vinyl etherHCID 8108—
反応物TriethylamineHCID 8471—
反応物5-Iodo-6-methyl-N-[4-(methylsulfonyl)benzyl]-2-oxo-1-[3-(trifluoro-methyl)phenyl]1,2-dihydropyridine-3-carboxamideHCID 11519933—
触媒Bis(1,2-bis(diphenylphosphino)ethane)palladium(0)HCID 2724231—
溶媒DimethylformamideHCID 6228—
生成物5-(1-Butoxyvinyl)-6-methyl-N-[4-(methylsulfonyl)benzyl]-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamideHCID 6672545628.5%

反応条件

温度100 °C

反応手順

5-Iodo-6-methyl-N-[4-(methylsulfonyl)benzyl]-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide (Example 1 (d), 101.5 mg, 0.17 mmol), bis[1,2-bis(diphenylphosphino)ethane]-palladium (0) (16.5 mg, 18.3 μmol), n-butyl vinyl ether (60 μl, 0.46 mmol), triethylamine (0.5 ml, 3.6 mmol) and DMF (6 ml) were placed in a Schlenk vessel equipped with a magnetic stirring bar. The vessel was purged with argon, sealed, and heated at 100° C. overnight. The reaction mixture was cooled and partitioned between ethyl acetate and water. The organic layer was dried over sodium sulphate, filtered and concentrated in vacuo. The residue was purified by preparative HPLC to give the title compound as a white solid (27.3 mg, 28%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08063073B2
出典データセットuspto-grants-2011_11
ORD IDord-f6f3ed1f69fb4c9a926f251a19a5551e
出典メモuspto-grants-2011_11