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)

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.

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.
 

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:
 

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.

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.

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

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.