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A straightforward and efficient synthesis of praziquantel enantiomers and their 4′-hydroxy derivatives
- Source :
- Tetrahedron: Asymmetry. 25:133-140
- Publication Year :
- 2014
- Publisher :
- Elsevier BV, 2014.
-
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.
Details
- ISSN :
- 09574166
- Volume :
- 25
- Database :
- OpenAIRE
- Journal :
- Tetrahedron: Asymmetry
- Accession number :
- edsair.doi...........1934756ead76a45f0d7d937fd1b7031e