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HRID 344379作成日:2026年10月27日

Toluene → 4-Amino-5-chloro-N-(1-(3-(2,3-dihydro-1,3-dioxo-1H-isoindol-2-yl)propyl)piperidin-4-ylmethyl)-2-methoxybenzamide

https://huagongshe.com/reaction/344379

反応式

関与物質

役割名称HCID仕込み量
反応物TolueneHCID 1140—
反応物Potassium CarbonateHCID 11430—
反応物4-BromopropylphthalimideHCID 23133286—
反応物4-Amino-5-chloro-2-methoxy-N-(piperidin-4-ylmethyl)benzamide hydrochlorideHCID 66780941—
溶媒DimethylformamideHCID 6228—
生成物4-Amino-5-chloro-N-(1-(3-(2,3-dihydro-1,3-dioxo-1H-isoindol-2-yl)propyl)piperidin-4-ylmethyl)-2-methoxybenzamideHCID 54150313—

反応条件

温度70 °C

反応手順

4-Amino-5-chloro-2-methoxy-N-(piperidin-4-ylmethyl)benzamide hydrochloride (8.0 g) was dissolved in dimethylformamide (100 ml) and toluene (100 ml). Potassium carbonate (9.9 g) and 4-bromopropylphthalimide (6.4 g) were added, and the mixture was stirred at 70° C. for 5 hr. The reaction mixture was concentrated under reduced pressure and the residue was extracted with ethyl acetate. The extract was dried over magnesium sulfate and concentrated under reduced pressure. The obtained residue was purified by silica gel chromatography to give 4.0 g of 4-amino-5-chloro-N-(1-(3-(2,3-dihydro-1,3-dioxo-1 H-isoindol-2-yl)propyl)piperidin-4-ylmethyl)-2-methoxybenzamide.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US05864039
出典データセットuspto-grants-1999_01
ORD IDord-6a3e8d330004481f8b19372b69962fa9
出典メモuspto-grants-1999_01