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HRID 907266作成日:2026年10月27日

Hydrochloric Acid → N-Cyclopropyl-3-(2-(4-hydroxybenzyl)-1-oxo-1,2-dihydroisoquinolin-6-yl)-4-methylbenzamide

https://huagongshe.com/reaction/907266

反応式

関与物質

役割名称HCID仕込み量
反応物Hydrochloric AcidHCID 313—
反応物Sodium HydroxideHCID 14798—
反応物Sodium hydrideHCID 24758—
反応物4-(Chloromethyl)phenyl acetateHCID 148312—
反応物N-Cyclopropyl-4-methyl-3-(1-oxo-1,2-dihydro-isoquinolin-6-yl)-benzamideHCID 25020457—
溶媒DimethylformamideHCID 6228—
生成物N-Cyclopropyl-3-(2-(4-hydroxybenzyl)-1-oxo-1,2-dihydroisoquinolin-6-yl)-4-methylbenzamideHCID 5755175281.5%

反応手順

To a solution of the product of Example 11 (460 mg) in DMF (10 mL) was added 60% sodium hydride (38 mg) and the reaction stirred at room temperature for 30 minutes before the addition of 4-(chloromethyl)phenyl acetate (280 mg). The reaction mixture was then stirred at room temperature for 17 hrs. Additional 60% sodium hydride (38 mg) was added and the reaction was stirred for a further 2 hours. NaOH (5N, 2 mL) was added and the reaction was stirred at room temperature for 90 minutes. The reaction mixture was acidified with HCl (2N) and extracted into ethyl acetate. The organics were washed with water and brine, dried over magnesium sulphate and evaporated to yield the sub-titled compound (500 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08012979B2
出典データセットuspto-grants-2011_09
ORD IDord-ab50e612b55a46608ff4714e6bba7b26
出典メモuspto-grants-2011_09