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HRID 504605作成日:2026年10月26日

Pyrrolidine → Z-2-[4-chloro-2-(6-chloro-5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-phenoxy]-2-ethyl-butyric acid methyl ester

https://huagongshe.com/reaction/504605

反応式

関与物質

役割名称HCID仕込み量
反応物PyrrolidineHCID 31268—
反応物6-Chloro-5-fluoroindolin-2-oneHCID 9794083—
反応物2-(4-Chloro-2-formyl-phenoxy)-2-ethyl-butyric acid methyl esterHCID 59428099—
溶媒MethanolHCID 887—
生成物Z-2-[4-chloro-2-(6-chloro-5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-phenoxy]-2-ethyl-butyric acid methyl esterHCID 86632112—

反応条件

温度70 °C

反応手順

To the mixture of 6-chloro-5-fluoro-1,3-dihydro-indol-2-one (500 mg, 2.7 mmol) and 2-(4-chloro-2-formyl-phenoxy)-2-ethyl-butyric acid methyl ester (844 mg, 2.97 mmol) in methanol (5 mL) was added pyrrolidine (95 mg, 1.35 mmol) dropwise. The mixture was then heated at 70° C. for 1 h. After cooled to room temperature, the mixture was partitioned between EtOAc and diluted HCl solution. The organic phase was washed with water, brine, dried over anhydrous Na2SO4 and concentrated to give the crude product as a red-yellow solid, which was used for the next step reaction without further purification.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07776875B2
出典データセットuspto-grants-2010_08
ORD IDord-127f6985906649c7a89aa6fa24ed79e0
出典メモuspto-grants-2010_08