Mi Sui-qing
2010
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Journal
Chinese Journal of New Drugs
Abstract
Objective: To synthesize 3-[4-(7-choloquinolin-4-yl) piperazin-1-yl] propanoic acid,an active metabolite of piperaquine.Methods: Piperazine was mono-protected with BOC,then reacted with ethyl 3-bromopropanoiate,subsequently deprotection,and substitution with 4,7-dichloroquinoline,and hydrolysis in consequence,afforded 3-[4-(7-choloquinolin-4-yl) piperazin-1-yl] propanoic acid.The target compound was further isolated and purified by silica gel chromatography.Results: 3-[4-(7-choloquinolin-4-yl) piperazin-1-yl] propanoic acid was synthesized successfully and the yield was 62.1%.The structure was confirmed by IR,1H-NMR,13C-NMR and HRMS.Conclusion: The synthesis method is simple,and the yield of 3-[4-(7-choloquinolin-4-yl) piperazin-1-yl] propanoic acid is high,so that it can be used for the synthesis of derivatives containing 4-piperazinyl quinoline ring.