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HRID 880676作成日:2026年10月27日

Potassium tert-butoxide → 4-(6-Fluoro-3,4-dihydro-1H-isoquinolin-2-yl)-2,6-dimethylphenyl-3,3-dimethyl butanamide

https://huagongshe.com/reaction/880676

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium tert-butoxideHCID 23665647—
反応物6-Fluoro-1,2,3,4-tetrahydroisoquinoline hydrochlorideHCID 45074042—
反応物N-(4-Bromo-2,6-dimethyl-phenyl)-3,3-dimethyl-butanamideHCID 59741059—
溶媒TolueneHCID 1140—
生成物4-(6-Fluoro-3,4-dihydro-1H-isoquinolin-2-yl)-2,6-dimethylphenyl-3,3-dimethyl butanamideHCID 86649628—

反応手順

Bis(dibenzylidineacetone)palladium (390 mg, 0.68 mmol) and (2′-dicyclohexyl phosphanyl-biphenyl-2-yl)-dimethylamine (800 mg, 2.0 mmol) were added to dry toluene (150 mL purged with argon for 30 minutes) and stirred for 30 minutes under argon. Potassium tert-butoxide (4.75 mg, 42.3 mmol), 6-fluoro-1,2,3,4-tetrahydro-isoquinoline hydrochloride salt (3.2 g, 17.0 mmol), and N-(4-bromo-2,6-dimethyl-phenyl)-3,3-dimethyl-butanamide (5 g, 16.8 mmol) were then added, and the reaction mixture was stirred at 80° C. overnight. The reaction mixture was then cooled to room temperature and recrystallized from toluene to afford the title compound as a solid. (5.11 g, 83%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08993593B2
出典データセットuspto-grants-2015_03
ORD IDord-2465b035f16a400ebdefc9548d845fee
出典メモuspto-grants-2015_03