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HRID 16421作成日:2026年10月24日

Ethyl Acetate → Benzenamine,4-[(6-chloro-3-methyl-1h-pyrrolo[2,3-b]pyridin-4-yl)oxy]-3-fluoro-

https://huagongshe.com/ja/reaction/16421

反応式

関与物質

役割名称HCID仕込み量
反応物Ethyl AcetateHCID 8857—
反応物Potassium CarbonateHCID 11430—
反応物Phenol, 4-amino-2-fluoro-HCID 2735918—
反応物1-acetyl-4,6-dichloro-3-methyl-1H-pyrrolo[2,3-b]pyridineHCID 17979289—
溶媒Dimethyl SulfoxideHCID 679—
生成物Benzenamine,4-[(6-chloro-3-methyl-1h-pyrrolo[2,3-b]pyridin-4-yl)oxy]-3-fluoro-HCID 17979286—

反応条件

温度120 °C

反応手順

300 mg (1.16 mmol) of 1-acetyl-4,6-dichloro-3-methyl-1H-pyrrolo[2,3-b]pyridine (from example XL) and 320 mg (2.32 mmol) of powdered potassium carbonate are suspended in 9 ml of DMSO. The mixture is degassed, and 442 mg (3.48 mmol) of 4-amino-2-fluorophenol are added. The mixture is heated at 120° C. for 4 hours. After addition of ethyl acetate, the mixture is filtered off with suction through CELITE (diatomaceous earth) and the filtercake is washed with ethyl acetate. The filtrate is extracted three times with sat. sodium bicarbonate solution and with sat. sodium chloride solution. The filtrate is dried over sodium sulfate and the solvent is removed under reduced pressure. The residue is purified by column chromatography (silica gel 60, mobile phase: DCM:methanol=50:1).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07737153B2
出典データセットuspto-grants-2010_06
ORD IDord-f54b7a1f971e4a7496946caf6e8bee25
出典メモuspto-grants-2010_06