Request for Help

A posting describing the skills and/or resources needed for a given project.

09 Oct

TCMDC-123812 and 123794, pending purification.

Published by pylioja

Subject 

Request for Help

I'm now fairly confident that I've made TCMDC-123794 and TCMDC-123812. By fairly confident I mean that I've got a reasonable looking but crude 1H NMR and low res. mass spec of both of the compounds. They are not clean by NMR after a column and the yield of the reaction was pretty bad (~20%). Still this isn't too bad for a first go, using a quick and dirty acid chloride. Most of the mass seems to go toward turning the acid into the anhydride.

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.

PZQ Manufacturing Capacity

Published by MikeGretes on 12 June 2010 - 1:04am

Subject 

Request for Help

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

Resolution of Praziquanamine

Published by MatTodd on 15 April 2010 - 8:43pm

Subject 

Request for Help

PZQ can't be resolved as-is (unless anyone has any bright ideas how to resolve amides). One of the most promising strategies to prepare enantiopure praziquantel (using a strategy that starts from the racemate) is a classical resolution of praziquanamine (1, "PZQamine").

Pictet-Spengler route to rac-PZQ

Published by Michael Wolfle on 15 January 2010 - 4:35am

Subject 

Request for Help

 
The synthesis of rac-PZQ via the Pictet-Spengler route was developed by the Korean Shin Poong Pharmaceutical Company and obtains very low production costs of US¢7 per 600 mg tablet of the drug.

A Summary of What is Needed Right Now

Published by MatTodd on 5 January 2010 - 8:42am

Subject 

Request for Help

Project A: Development of a low-cost enantioselective synthesis of PZQ. It's an open project, like everything on TSL.
Meaning?: contributors can change anything they wish on these pages.
If you wish to contribute: please don't leave comments here. Instead, edit the pages below directly or leave comments.

Starting Materials for the Synthesis of rac-PZQ

Published by Michael Wolfle on 5 January 2010 - 8:27am

Subject 

Request for Help

 
For an inexpensive route to rac-PZQ (and potentially the enantioenriched material), the relevant starting materials (below) are required. While prices may be obtained for these from commercial catalogues, we require realistic prices of these materials on a large (ton) scale to assess whether this approach to PZQ is economically viable. The starting materials are:
 

Reissert Approach to rac-PZQ

Published by Michael Wolfle on 5 January 2010 - 8:25am

Subject 

Request for Help

The most obvious, and known, approach to rac-PZQ is using Reissert chemistry.
 
 
This approach has been used in the following publications:
 [1]    Organic Sonochemistry. Synthesis and Use of Reissert compounds under PTC-Ultrasound, J. Ezquerra and J. Alvarez-Builla, J. Heterocyclic Chem. 1988, 25, 917-925.

13 Oct

Frustration with recrystallization

Published by RyanPakula

Subject 

Request for Help

Last Wednesday I began some simple tests to try to find a good solvent for recrystallization, and here's some details and thoughts on what I've found so far.

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