Ethyl piperazine-1-acetate → Ethyl [4-(1,1-Dimethyl-2-oxo-ethyl)-piperazin-1-yl]-acetate

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Reaction Steps

A solution of 100 g 2-bromo-2-methyl-propionaldehyde in 20 ml of ethanol is added dropwise to a mixture of 25.0 g N-[(ethoxycarbonyl)methyl]-piperazine in 80 ml of ethanol at room temperature. The resulting mixture is stirred for 72 hours, concentrated in vacuo, and submitted directly to column chromatography on silica gel with methylene chloride/methanol (95:5 to 80:20) to give the title compound as a yellow oil. Yield: 10.0 g (62% of theory), Rf value: 0.60 (silica gel, methylene chloride/methanol=9:1) Mass spectrum (ESI*): m/z=241 [M−H]*

Provenance & Evidence