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HRID 58702作成日:2026年10月24日

Diisopropylethylamine → N-(2-(5-chloro-1H-indol-3-yl)ethyl)-1-(2-fluorophenyl)-2-oxopyrrolidine-3-carboxamide

https://huagongshe.com/ja/reaction/58702

反応式

関与物質

役割名称HCID仕込み量
反応物DiisopropylethylamineHCID 81531—
反応物PyBOPHCID 2724699—
反応物5-Chloro-1H-indole-3-ethylamine monohydrochlorideHCID 2827494—
反応物1-(2-Fluorophenyl)-2-oxo-3-pyrrolidinecarboxylic acidHCID 4569153—
溶媒DimethylformamideHCID 6228—
生成物N-(2-(5-chloro-1H-indol-3-yl)ethyl)-1-(2-fluorophenyl)-2-oxopyrrolidine-3-carboxamideHCID 6683190644%

反応手順

A mixture of 2-(5-chloro-1H-indol-3-yl)ethanamine hydrochloride (0.104 g; 0.448 mmol), PyBOP (0.349 g; 0.672 mmol), N,N-diisopropylethylamine (0.232 mL; 1.34 mmol) and 1-(2-fluorophenyl)-2-oxopyrrolidine-3-carboxylic acid (0.100 g; 0.448 mmol) was stirred in DMF (3 mL) overnight. The reaction mixture was partitioned between ethyl acetate and sodium hydrogen sulfate, the organic layer was washed with sodium carbonate, brine, dried and concentrated under reduced pressure. The crude mixture was purified flash chromatography on silica (eluent 20 to 100% ethyl acetate in heptane) to yield 0.078 g (44%) of the title compound as a white solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09434722B2
出典データセットuspto-grants-2016_09
ORD IDord-b844dc2284db47c68ffbd974f6f073b6
出典メモuspto-grants-2016_09