We started catalyst screenings for the asymmetric Pictet-Spengler reaction. So far, we have tested several achiral Brønsted-acidic catalysts to determine acid strength which is required to cyclize the open-chain praziquantel intermediate 1 to the tetrahydroisoquinoline heterocycle 2.
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 goo
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
Following link will be where requirements are documented. (This should support anonymous access).
To host the raw data from the Pictet-Spengler approach to the enantioselective synthesis of PZQ Michael has started an Electronic Lab Notebook. We're using the open source Southampton Lab Blog interface for this, since we're collaborating with them on a couple of things related to this site.
Syncom B.V., The Netherlands, a CRO specialized in all aspects of organic synthesis, with a 20-year track record in resolution of chiral compounds, screened five different chiral HPLC columns, varied the eluent and used UV detection (220 and 260 nm) and a PDR-Chiral Advanced Laser Polarimeter.
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