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content appropriate for schistosomiosis research

06 May

Help from the Process Sector

Published by MatTodd

It's been a great week for the PZQ project, since we've had an injection of real help from the people we most need - process chemists. Much of this has arisen from a discussion I started on LinkedIn, which then became emails, but all participants have either actively participated on this site, or granted permission for the posting of information here.

Suggested conditions

Published by ndt228 on 6 May 2010 - 7:36pm

Dear Matt,
This may come too late, but you could look into using conditions published by AGMBarrett for aliphatic nitro group reductions, by transfer hydrogenation.  Its in Tet Lett but there's an open-access link here:
http://www.erowid.org/archive/rhodium/chemistry/nitro2amine.cth.pd-af.html
regards
Nick

The Drug Development Process

Published by ndt228 on 2 May 2010 - 7:01pm

Subject 

Miscellaneous

There may be members of this community who do not yet have direct experience of developing a new medicine from concept to pharmacy shelf.  Be assured, there is a lot more to it than "just" the synthesis of the API.  Why not take advantage of a Free ACS Webcast on May 6, 2010 Thurs 2:00-3:00 PM ET
From a Beaker to a Bottle: Overview of the Drug Discovery and Development Process for Small Molecule Therapeutics

Resolution of PZQAmine

Published by ndt228 on 2 May 2010 - 9:34am

I'd like to suggest that this approach deserves its own thread - at present it is mentioned within the stereoselective synthesis project.  I think it is more important than that - if you agree, there is existing content that should be migrated across to here. 

Resolutions of PZQ

Published by Ahamed on 1 May 2010 - 11:20pm

Analytical chromatography
There are many ways to analyse PZQ with enantioselective chromatography. The approach used in-house at Sydney.  We used ChiralcelOD-H column, Solvents: Hex:IPA:TEA 60:40:0.1, Flow Rate: 0.7 mL/min. The retention times were 12.362  & 14.932 mins. Sample HPLC trace is posted below.
Preparative chromatography
Paper detailing the preparative separation of PZQ enantiomers by Intervet:

Genetic similarity of S. haematobium and S. mansoni?

Published by perforin on 27 April 2010 - 3:34pm

Hi All,
Anyone have an estimate of the genetic similarity between S. haematobium and S. mansoni? I have not been able to locate a figure.
Thanks,
Mike

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").

Synthetic alternatives to PZQ

Published by MatTodd on 1 April 2010 - 1:53am

Synthetic compounds that are alternatives to PZQ - anyone can assemble a list below.

Naturally-occurring alternatives to PZQ

Published by MatTodd on 1 April 2010 - 12:08am

To assemble a list below of naturally-occurring alternatives to PZQ for the treatment of schistosomiasis.

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