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HRID 42186作成日:2026年10月26日

Sodium Carbonate → 6-[(R)-4-(4-Benzylphthalazin-1-yl)-2-methylpiperazin-1-yl]nicotinonitrile

https://huagongshe.com/reaction/42186

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium CarbonateHCID 10340—
反応物6-Chloro-3-pyridinecarbonitrileHCID 5152094—
反応物1-Benzyl-4-((R)-3-methyl-piperazin-1-yl)-phthalazineHCID 44186248—
溶媒DimethylformamideHCID 6228—
溶媒1,4-DioxaneHCID 31275—
生成物6-[(R)-4-(4-Benzylphthalazin-1-yl)-2-methylpiperazin-1-yl]nicotinonitrileHCID 4418648042.2%

反応手順

Solid Na2CO3 (50 mg, 0.47 mmol, 1.5 eq) is added to a solution of 6-chloronicotinonitrile (50 mg, 0.36 mmol, 1.2 eq), 1-benzyl-4-((R)-3-methyl-piperazin-1-yl)-phthalazine (100 mg, 0.31 mmol, 1.0 eq) in DMF (1 mL) and dioxane (2 mL) in a microwave vial. The vial is sealed and irradiated in the microwave at 180° C. (high absorption setting) for 30 minutes. The reaction mixture is concentrated, dichloromethane is added and is washed with water then brine. The organic fraction is dried over sodium sulfate, and is evaporated under reduced pressure, then purified by flash chromatography (50%-90% EtOAc/Hexane) to afford the title compound as a white solid (55 mg, 42% yield).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08536168B2
出典データセットuspto-grants-2013_09
ORD IDord-0ba5931c41c24e159e704285350d2dc6
出典メモuspto-grants-2013_09