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02 Dec

Two weeks in the PZQ lab

Published by KatB

Subject 

Rants, Miscellaneous

 
I've now reached the end of my second week in the lab working on the Pictet-Spengler route to praziquantel.
 

XRPD patterns of rac- and (R)- PZQAmine

Published by ndt228 on 6 October 2011 - 8:33pm

The attached file contains X-ray powder diffraction patterns (XRPDs) for racemic and (R)- PZQAmine, as well as a mixture of the two.  These confirm that (as is often the case) the racemic compound and the single enantiomer have different crystal structures.  This is consistant with the phase diagram for PZQ Amine gathered from the melting point of mixtures of the two.
Thanks to Jana Galbraith (Almac Sciences Physical Sciences Dept) for recording these patterns.

Characterisation of rac- and (R)- PZQ Amine

Published by ndt228 on 5 October 2011 - 10:06pm

A start has finally been made on determining the phase diagram for PZQAmine from 0 to 100% ee, based upon melting point determination of known % w/w mixtures of racemicand single enantiomer PZQAmine.  Samples of the latter were provided by Michael early this year. 

21 Sep

First Full Paper on a TSL Project

Published by MatTodd

Subject 

Miscellaneous

The first paper arising from the open science coordinated by this site has just been published here. Though the project is very much ongoing, it's super exciting to be able to publish a paper as a milestone. i.e. one can run an open project, and once a certain point has been reached, one can submit a paper for traditional peer review to act as a reviewed summary of progress.
 

Student Optimization of PZQ Resolution

Published by MatTodd on 24 March 2011 - 12:01pm

Subject 

Request for Help

This page is intended as a place where people can discuss the student-led optimization of PZQ resolution. Relevant ELN is here, containing background here. Description of how students can help out is here (PDF). Paper will be assembled here.

09 Mar

Doemling's Chiral Praziquantel Synthesis????

Published by CreativeChemistry

 While Doemling has published (and patented) a Ugi approach to racemic PZQ, there was also a claim in an abstract from a ASTMH meeting from December 2008 that he was to talk about a chiral synthesis (abstract below). Anyone know anything about this?
 

Sandbox for Synthetic Ideas

Published by MatTodd on 30 January 2011 - 7:49am

This is a post of random synthesis ideas for praziquantel that have been sitting in my inbox for too long. Both sources are industrial. If anyone has any comments, please post. If anyone has any further ideas, please post directly here – you can see how long it can take things to emerge if you use email...
 

25 Jan

Praziquantel Update January 25 2011

Published by MatTodd

The resolution of PZQ via PZQamine is working very nicely on a gram scale. We're still tweaking and improving it. For example the initial resolving agent identified by Syncom, dianisoyl tartaric acid, can be replaced by dibenzoyl tartaric acid. The latter is easier to purify, is less expensive (to buy and probably to make) and gives the opposite (desired!) enantiomer of PZQamine in the solid. The resolving agent can also be easily recycled in good yield.

06 Dec

Development of OSDD business model - assistance wanted

Published by clarson

We (at the Norwegian Knowledge Center for Health Services) are attempting to create an open source drug discovery business model that will hopefully assist individuals interested in undertaking such a project. Once the model is created, it will be made freely available. (You can read more about our project at www.kunnskapssenteret.no/osdd.) To build this model, we would like to learn from you about your experiences at the Synaptic Leap.

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