Objective To improve the poor water solubility and low bioavailability of tetrandrine and its clinical applications.Methods The synthetic routes of tetrandrine derivatives were designed.The target derivatives were obtained by nitration reactions,reduction reactions,amide condensation reactions,click chemistry,and elimination reactions with tetrandrin as the starting point.All the derivatives were elucidated by ESI-MS,1H NMR,and 13C NMR spectra.The aqueous solubility of selected compounds were evaluated.Results Totally 10 glycoside tetrandrine derivatives and one C-14 amide tetrandrin derivatives were first synthesized.Conclusion The water solubility of the glycoside tetrandrine derivatives is greatly improved,and compound 1b,the tetrandrin maltose derivative,exhibits notable water solubility for further research.
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