MatTodd's blog

09 Mar

Deuterated PZQ

Published by MatTodd

Subject 

Miscellaneous

Was alerted to this NCTT project/proposal for deuterated analogs of enantiopure PZQ, with the deuteration being used to slow metabolism. Would be interesting to see how many D's are incorporated, and where (presumably at least the 4' position). I hope they're using our resolution approach to make their enantiopure material. And I wonder what the deuteration does to the cost, on scale?
(original page http://nctt.nih.gov/27545311)

17 Oct

Where Else Have the Aryl Pyrroles been Evaluated?

Published by MatTodd

Subject 

Miscellaneous

Last week I was talking with Lei Liu from Tsinghua University, who was visiting Sydney to give a talk on his synthetic methodology research. I showed him the compounds that are the starting point of the open source drug discovery project for malaria, the arylpyrrole set.

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.
 

17 Sep

Patents, Universities and Open Source

Published by MatTodd

Community 

general open research

Subject 

Miscellaneous

Saw this very interesting article/development. Intel sponsoring research at top universities, but heavily encouraging the projects to be open source and the universities not to take out patents. A bold step, very counter to the philosophy that is so familiar to any current academic. From the website:
 

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.

08 Nov

Summary November 8th 2010

Published by MatTodd

We now have two resolutions of PZQ! (or, more correctly, PZQ precursors) The previously-posted resolution (A, see scheme below) involves taking PZQ itself, removing the cyclohexanoyl group to give PZQamine, resolving this amine with a derivative of tartaric acid, then re-introducing the cyclohexanoyl group.

20 Oct

Praziquantel Update October 20th 2010

Published by MatTodd

A lot has been happening here in the last few weeks, so I ought to summarise:

11 Aug

Ignite Sydney talk on Open Science and TSL

Published by MatTodd

Community 

general open research

I recently gave a talk on open science at Ignite Sydney. These talks are a real challenge in that you have 5 minutes to get across an idea, with the slides rotating every 15 seconds behind you. The event was in a cool club/gallery in the middle of Sydney, and is the first talk I've ever given where I was preceded by a beatbox act. Apparently I was the first scientist to go to Ignite Sydney.
 

25 May

New ELN for Pictet-Spengler Approach

Published by MatTodd

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.
 

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