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HRID 5106作成日:2026年10月24日

Formaldehyde → (2S, 4S)-2-Ethylcarbamoyl-4-(4-methoxybenzylthio)-1-methylpyrrolidine

https://huagongshe.com/reaction/5106

反応式

関与物質

役割名称HCID仕込み量
反応物FormaldehydeHCID 712—
反応物Sodium ChlorideHCID 5234—
反応物Sodium HydroxideHCID 14798—
反応物Sodium cyanoborohydrideHCID 5003444—
反応物(2S, 4S)-2-Ethylcarbamoyl-4-(4-methoxybenzylthio)pyrrolidineHCID 14880286—
溶媒AcetonitrileHCID 6342—
生成物(2S, 4S)-2-Ethylcarbamoyl-4-(4-methoxybenzylthio)-1-methylpyrrolidineHCID 1059094278.1%

反応手順

3.43 ml of 35% formalin and 804 mg of sodium cyanoborohydride were added to a solution of 2.36 g of (2S, 4S)-2-ethylcarbamoyl-4-(4-methoxybenzylthio)-pyrrolidine dissolved in 42 ml of acetonitrile, and the mixture was stirred at room temperature for 40 minutes. At the end of this time, a 1N aqueous solution of sodium hydroxide was added, and the reaction mixture was poured into an aqueous solution of sodium chloride and extracted with ethyl acetate. The extract was washed with an aqueous solution of sodium chloride and dried over anhydrous magnesium sulfate, and the solvent was removed by distillation under reduced pressure. The residue was purified by column chromatography through silica gel (eluted with ethyl acetate) to afford 1.93 g of the title compound as colorless crystals.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US05242914
出典データセットuspto-grants-1993_09
ORD IDord-0396738389f34b4993d50a9f35e708e2
出典メモuspto-grants-1993_09