The Synaptic Leap

 I came upon this reference:
http://www3.interscience.wiley.com/journal/123349682/abstract
which refers to masking of bitter taste of an API through formulation with a beta-cyclodextrin derivative.

Based on past experience with "Chiral Switch" projects in a commercial environment, I have drafted the attached document as a summary of my understanding of the aims of the PZQ project in the context of what would be needed (technically) to get (R)-PZQ to market in the western world.  This does not examine manufacture per se, but rather the many necessary steps to obtain permission to market.  I am sure there are some which I may have missed, but the point is that there would (in my past experience) be far more going on than focussing as at present on "manufacture" and "cost of goods", however important these will be in the long-run. 

Let's think long-term: How best to scale up production of PZQ?

This is likely most economically done in India or China (possibly Brazil or South Africa), all of which have well-established pharmaceutical manufacturing sectors.  However, building manufacturing capacity in poorer disease-endemic countries stands to have enormous benefits for economic development and potential to eventually better meet local and regional general pharmaceutical demand! 

 

 
Here is a procedure from a German Patent Application from 1975 which uses quinic acid for the racemic resolution of praziquanamine. However, the procedure gives less information about the yield obtained.
 

A new patent application using a multistep reaction (Ugi reaction) for the synthesis of Praziquantel
 

 

Project to determine if it is feasible to automate / accelerate the catalyst screening project through automated software systems. 
Currently the project is in requirements initiation. We are defining top level requirements of what an automated tool will look like.  Please feel free to contribute

Welcome, I'm Mat Todd, the community leader for schistosomiasis research. If you're looking for the PZQ project - shortcut here.

This page details attempts to optimise the recrystallization of praziquantel. Anybody can add to/edit this page.
 
Literature
1. This patent (US patent 4,523,013) recrystallizes PZQ from "a mixture of petroleum ether and acetone," obtaining a 95% yield on the reaction.
2. This paper recrystallizes from ethyl acetate and hexanes to obtain a 70% yield on the reaction.
 
The best system the Todd lab has observed for the recrystallization of racemic praziquantel, as of Oct. 26, 2009, is the following: