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HRID 229860作成日:2026年10月26日

p-Toluenesulfonic acid → 2-methyl-1-[(S)-1-(tetrahydro-furan-2-yl)methyl]-5-(2-trifluoromethoxy-phenyl)-1H-pyrrole-3-carboxylic acid methyl ester

https://huagongshe.com/reaction/229860

反応式

関与物質

役割名称HCID仕込み量
反応物p-Toluenesulfonic acidHCID 6101—
反応物(S)-(+)-TetrahydrofurfurylamineHCID 641530—
反応物3-Oxo-2-[2-oxo-2-(2-trifluoromethoxy-phenyl)-ethyl]-butyric acid methyl esterHCID 69021229—
溶媒MethanolHCID 887—
生成物2-methyl-1-[(S)-1-(tetrahydro-furan-2-yl)methyl]-5-(2-trifluoromethoxy-phenyl)-1H-pyrrole-3-carboxylic acid methyl esterHCID 69023243—

反応手順

To a solution of 250 mg of 3-oxo-2-[2-oxo-2-(2-trifluoromethoxy-phenyl)-ethyl]-butyric acid methyl ester in methanol was added 84 μl of (S)-tetrahydrofurfurylamine and 5 mg of p-toluene sulfonic acid. The reaction mixture was then heated at reflux for 24 hours. After such time the reaction mixture was allowed to cool to room temperature before being concentrated in vacuo and purified by column chromatography to give 171 mg of the title compound; MS (EI) 383.1 (M)+.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07563910B2
出典データセットuspto-grants-2009_07
ORD IDord-4a5cf6c4afb64be6b49837ecfc880f33
出典メモuspto-grants-2009_07