CHENG Xun-guan, ZHENG Xiao-hong, XIA Zhu, et al. A new and efficient method for the synthesis of praziquantel,an antischistosomiasis drug[J]. Journal of Chongqing Medical University, 2011,36(10):1208-1210.
CHENG Xun-guan, ZHENG Xiao-hong, XIA Zhu, et al. A new and efficient method for the synthesis of praziquantel,an antischistosomiasis drug[J]. Journal of Chongqing Medical University, 2011,36(10):1208-1210.DOI:
Objective:To establish an industrial synthetic route for praziquantel.Methods:Praziquantel was synthesized with an overall yield of about 32.8% from phenylethylamine via acylation
amination with phthalimide potassium
Bischler-Napieralski cyclization
hydrazine solution
reduction
followed by acylation with cyclohexanecarboxylic acid chloride and chloroacetyl chloride
and then cyclization.Results:Target structures werecharacterized by IR
UV and MS.Conclusion:The method has the advantages of convenient operation
mild reaction conditions and high yield.This method is fit for industrial process.