87693-75-2Relevant articles and documents
A concise and highly efficient synthesis of praziquantel as an anthelmintic drug
Yang, Zhezhou,Zhang, Lin,Jiao, Huirong,Bao, Rusheng,Xu, Weiwei,Zhang, Fuli
, p. 1983 - 1993 (2016/11/26)
A concise and practical synthesis of praziquantel as anthelmintic drug is described. The key steps include a monoalkylation of ethanolamine for the preparation of 2-(2-hydroxyethylamino)-N-phenethylacetamide and a mild oxidation protocol with SO3-Py/DMSO as oxidant to transform alcohol into the corresponding aza-acetal. The telescoped synthesis is composed of five steps without purification of the intermediates, providing an overall yield of 80% with 99.8% purity after crystallization.
NEW SYNTHESES OF PRAZIQUANTEL : 2-(CYCLOHEXYLCARBONYL)-1,2,3,6,7,11b-HEXAHYDRO-4H-PYRAZINOISOQUINOLIN-4-ONE
Frehel, Daniel,Maffrand, Jean-Pierre
, p. 1731 - 1735 (2007/10/02)
This paper describes two different synthetic pathways for praziquantel, a new broad spectrum schistosomicide and cestocide.Easy to apply on an industrial scale, they involve a selective reduction of 4-acyl-1-phenethylpiperazine-2,6-dione in 4-acyl-6-hydroxy-1-phenethylpiperazin-2-one, the cyclisation of wchich in acetic medium gives tricyclic compounds 2-acyl-1,2,3,6,7,11b-hexahydro-4H-pyrazinisoquinolin-4-one.