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Saturday, 29 October 2016

A Concise and Highly Efficient Synthesis of Praziquantel as an Anthelmintic Drug








PAPER

HETEROCYCLES

An International Journal for Reviews and Communications in Heterocyclic Chemistry
Web Edition ISSN: 1881-0942

Published online: 11th October, 2016

Paper | Regular issue | Prepress
DOI: 10.3987/COM-16-13538
■ A Concise and Highly Efficient Synthesis of Praziquantel as an Anthelmintic Drug
Zhezhou Yang, Lin Zhang, Huirong Jiao, Rusheng Bao, Weiwei Xu, and Fuli Zhang*
*Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, 285 Gebaini Road, Shanghai 201203, China
Abstract
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.


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