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HRID 10580作成日:2026年10月26日

4-Methoxybenzylamine → 4-[1-(4-Methoxybenzyl)amino-5-isoquinolyl]amino-1-(tert-butoxycarbonyl)piperidine

https://huagongshe.com/reaction/10580

反応式

関与物質

役割名称HCID仕込み量
反応物4-MethoxybenzylamineHCID 75452—
反応物2-(Di-tert-butylphosphino)biphenylHCID 2734215—
反応物4-(1-Chloro-5-isoquinolyl)amino-1-(tert-butoxycarbonyl)piperidineHCID 21979829—
反応物Sodium t-butoxideHCID 23676156—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒TolueneHCID 1140—
生成物4-[1-(4-Methoxybenzyl)amino-5-isoquinolyl]amino-1-(tert-butoxycarbonyl)piperidineHCID 21979935—

反応条件

温度70 °C

反応手順

A suspension of Intermediate 84 (235 mg), 4-methoxybenzylamine (110 μl), tris(dibenzylideneacetone)dipalladium(0) (30.4 mg), 2-(di-tert-butylphosphino)biphenyl (41.0 mg) and sodium tert-butoxide (93.6 mg) in toluene (4.5 ml) was stirred at 70° C. for 1 hour. The reaction mixture was filtered through a Celite layer, and the solvent was evaporated under reduced pressure. Then, the residue was purified by silica gel column chromatography (n-hexane:ethyl acetate=3:1) to obtain the title compound (270 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07094789B2
出典データセットuspto-grants-2006_08
ORD IDord-d189c45fbcf042a78bf55612f254a951
出典メモuspto-grants-2006_08