Hu Yang
2010
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Journal
Chinese Journal of Medicinal Chemistry
Abstract
Aim To improve the synthetic procedure of plerixafor.Methods Plerixafor,an anti-tumor agent was synthesized from diethyl malonate by aminolysis with ethylenediamine,Michael reaction with methyl acrylate and cyclization to give 1,4,8,11-tetraazacyclotetradecane-5,7,12-trione,followed by condensation with α,α′-dibromo-p-xylene,and reduction.Results and conclusion The structure of target compound was confirmed by 1H-NMR and MS spectra,and the overall yield was 27.5%.The improved process is easy for synthesis and suitable for industrial manufacturing owing to its advantages of low cost,convenient operations without column chromatography.