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HRID 57744作成日:2026年10月24日

Hydrochloric Acid → Diethyl 2-benzyloxycarbonylamino-2-(t-butoxycarbonylmethyl)malonate

https://huagongshe.com/ja/reaction/57744

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Potassium CarbonateHCID 11430—
反応物tert-Butyl bromoacetateHCID 79177—
反応物Diethyl 2-(benzyloxycarbonylamino)malonateHCID 259787—
触媒Potassium IodideHCID 4875—
溶媒DimethylformamideHCID 6228—
生成物Diethyl 2-benzyloxycarbonylamino-2-(t-butoxycarbonylmethyl)malonateHCID 66725345100.8%

反応条件

温度50 °C

反応手順

A suspension of diethyl 2-benzyloxycarbonylaminomalonate (5.0 g), potassium carbonate (2.7 g), potassium iodide (0.27 g), and t-butyl 2-bromoacetate (4.1 g) in DMF (50 mL) was stirred at 50° C. for 1 hour. The reaction mixture was cooled, and then poured into diluted hydrochloric acid, the mixture was extracted with ethyl acetate, and the extract was washed with saturated brine, and then dried over anhydrous magnesium sulfate. The solvent was evaporated under reduced pressure, and the residue was subjected to silica gel column chromatography, and then purification was performed with n-hexane/ethyl acetate (5:1), to obtain the title compound (6.9 g, yield: 99%) as colorless oil.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09434737B2
出典データセットuspto-grants-2016_09
ORD IDord-90797a7338924070b568b0d13d20c8a2
出典メモuspto-grants-2016_09