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Start Over Descriptor "Praziquanamine" Publisher elsevier bv
1 results on '"Praziquanamine"'

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

Author

María Isabel Aguilar, Alberto Cedillo-Cruz, Marcos Flores-Alamo, Helgi Jung-Cook, and Francisca Palomares-Alonso

Subjects
Praziquanamine, Cyclohexane, Stereochemistry, Organic Chemistry, Cyclohexanecarboxylic acid, Catalysis, Inorganic Chemistry, Praziquantel, chemistry.chemical_compound, Residue (chemistry), chemistry, Hydrogenolysis, medicine, Physical and Theoretical Chemistry, Enantiomer, medicine.drug
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 of the compounds was tested, finding that (R)-(−)-praziquantel is the eutomer.

Published
2014

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