A straightforward and efficient synthesis of praziquantel enantiomers and their 4′-hydroxy derivatives

…, MI Aguilar, M Flores-Alamo, F Palomares-Alonso…

Index: Cedillo-Cruz, Alberto; Aguilar, Maria Isabel; Flores-Alamo, Marcos; Palomares-Alonso, Francisca; Jung-Cook, Helgi Tetrahedron Asymmetry, 2014 , vol. 25, # 2 p. 133 - 140

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Abstract

Abstract A new method for the synthesis of praziquantel enantiomers via resolution of praziquanamine with (S)-(+)-naproxen was developed. The four 4′-hydroxy derivatives were obtained through each single praziquanamine enantiomer, coupling with cis-and trans- 4-(benzyloxy) cyclohexanecarboxylic acids and subsequent hydrogenolysis for the deprotection of the 4′-OH cyclohexane residue. Additionally, the in vitro cysticidal activity ...

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