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HRID 30186作成日:2026年10月24日

Hydrochloric Acid → 1-Fmoc-4-Boc-Piperazine-2-acetic acid

https://huagongshe.com/ja/reaction/30186

反応式

関与物質

役割名称HCID仕込み量
反応物Hydrochloric AcidHCID 313—
反応物9-Fluorenylmethyl chloroformateHCID 34367—
反応物Methyl 4-Boc-piperazine-2-acetateHCID 2756816—
溶媒Sodium HydroxideHCID 14798—
生成物1-Fmoc-4-Boc-Piperazine-2-acetic acidHCID 2756796—

反応条件

温度5 °C

反応手順

3-Methoxycarbonylmethylpiperazine-1-carboxylic acid tert-butyl ester (6.0 g) was dissolved in TBF (60 ml) and 1N sodium hydroxide solution (60 ml) and stirred at room temperature for 6 hours. The solution was then cooled to 5° C. and adjusted to pH 9-10 by the addition of 10% hydrochloric acid. Nα(9-Fluorenylmethoxycarbonyl chloride (6.05 g) was then added portionwise, maintaining the pH at 9-10 by the addition of 1N NaOH solution. The reaction mixture was stirred at 5° C. for 16 hours. The solution was then adjusted to pH 1 by the addition of 10% hydrochloric acid. The solution was extracted with ethyl acetate (×2), dried (MgSO4) and evaporated. The title compound was obtained as a white foam (9.96 g), mass spectrum (API+) 411 [(M-C4H8)H+], C26H30N2O6 requires 466.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07423052B2
出典データセットuspto-grants-2008_09
ORD IDord-bd2c7ff1f3a949b6b56b20e3ea0f6d2b
出典メモuspto-grants-2008_09