Computed Properties of C13H14ClN3. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 7-Chloro-4-(piperazin-1-yl)quinoline, is researched, Molecular C13H14ClN3, CAS is 837-52-5, about Synthesis of hydroxypiperaquine, an antimalarial drug. Author is Thai, Hoang; Nguyen, Thac Kim; Nguyen, The Anh.
Piperaquine has been effectively used in combination with dihydroartemisinin for the treatment of the CQ-resistant malaria in Vietnam. At present, this compound is synthesized in our laboratory on multikilogram scale for making the drug artekin for the treatment of malaria. In this paper, we describe the synthesis of hydroxypiperaquine, a derivative of piperaquine. Hydroxypiperaquine is a known antimalarial drug. Hydroxypiperaquine was synthesized by two methods. In the first method, hydroxypiperaquine was synthesized in 50% yield by treatment of two equivalent of 7-chloro-4-(piperazin-1-yl)quinoline with one equivalent of epichlorohydrin. In the second method, hydroxpiperaquine was obtained in 70% yield by reaction of 7-chloro-4-(piperazin-1-yl)quinoline with 1-chloro-3-[4-(7-chloroquinolin-4-yl)piperazin-1-yl]propan-2-ol. The structures of the intermediates and hydroxypiperaquine were reconfirmed by IR, MS and NMR spectra.
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