Todd:PZQ Student Optimization
Student-led Optimization of the Resolution of Praziquantel
New authors - add yourselves here in alphabetical order:
Piero Olliaro, Special Programme for Research and Training in Tropical Diseases (TDR), World Health Organization, Avenue Appia 20, 1211 Geneva 27, Switzerland
Matthew H. Todd, School of Chemistry, The University of Sydney, NSW 2006, Australia
Michael Woelfle, School of Chemistry, The University of Sydney, NSW 2006, Australia
Authors have contributed to the open electronic lab notebook where the original research was first disclosed.
Abstract
A preparation of enantiopure praziquantel was recently discovered that involves the classical resolution of a hydrolysis product, praziquanamine. The protocol is experimentally simple, and involves no chromatography. For the procedure to be of the greatest impact, the price must be kept very low, meaning that the process must be highly optimized. This paper describes the results obtained by a distributed group of students working on this problem in an open source manner.
Introduction
Description of schisto, PZQ and the need for (R)-PZQ
Description of the existing process
Identification of current shortcomings
Brief outline of how the project was intended to operate
Results and Discussion
Chemistry
How the collaboration worked
Methods and Materials
Hydrolysis of PZQ
Synthesis of Resolving Agents
The Resolution of PZQamine
Conversion of PZQamine to PZQ
References
(Please include DOIs to any references provided)
