摘要 |
The present invention provides a novel process for easily and affordably obtaining (R)-(-)-praziquantel, (S)-(+)-praziquantel, as well as a process for the synthesis of the main hydroxylated metabolites thereof. The process of the present invention involves the resolution of the praziquanamine 12, 3, 6, 7 11b-hexahydro-4h-pyrazine [2,1-a]isoquinoline-4-ona, with (S)-(+)-naproxen as a resolution agent; while the synthesis of the stereoisomers cis and trans-4’-hydroxylated of (R)-(-)-praziquantel is performed from the mixture of cis and trans-4’hydroxy cyclohexanecarboxylate of ethyl and the (R)-(-)-praziquinamine. |