Resynthesis of MMV670652 and separation of enantiomers.

[alintheopen]

MMV670652 was a promising candidate from the briefing document (/data/7353.html) and should be resynthesised and the enantiomers separated by prep HPLC. Will need to find a collaborator to assist with separation.

[PatrickThomson]

The briefing document seems unclear - it reads like they currently have one enantiomer and think the other one might be better? Or was it screened as a racemate? I could potentially have one of my students take this as a project (one's on amide linkers, the other on alcohol linkers).

[mattodd]

If the enantiomers are to be evaluated in Australia, it would be slightly
preferable to make the racemate here too. The options for prep HPLC are:

1. The facility at the University of Queensland (
   http://researchers.uq.edu.au/research-project/9959). This will probably,
   based on past experience, cost money. I can enquire.
2. A separation by Phenomenex (http://www.phenomenex.com/) who have
   previously expressed an interest in the project's open science nature.
3. A separation by Merck, New Jersey, who have also expressed an interest
   in open work and recently made a fantastic job of enantiomer separation for
   Kat Badiola's open catalysis project (data not yet uploaded...)
4. A service based in Europe, perhaps in the UK/Geneva - suggestions
   welcome.

In all cases we'd want to be exploring gratis/in kind contributions rather
than those requiring a fee.

On 11 November 2013 10:45, PatrickThomson [email protected] wrote:

The briefing document seems unclear - it reads like they currently have
one enantiomer and think the other one might be better? Or was it screened
as a racemate? I could potentially have one of my students take this as a
project (one's on amide linkers, the other on alcohol linkers).

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[JoieG]

For clarification - MMV670652 was tested as a racemate. It would be beneficial to find a collaborator to separate the enantiomers in order to understand the activity and stability of each enantiomer. Is someone responsible for reaching out to these contacts listed by Mat and inquiring about willingness to help?

[mattodd]

Yes, that's me, but I want to ensure we're not overlooking another source
of separation expertise beyond this current list.

On 11 November 2013 23:11, JoieG [email protected] wrote:

For clarification - MMV670652 was tested as a racemate. It would be
beneficial to find a collaborator to separate the enantiomers in order to
understand the activity and stability of each enantiomer. Is someone
responsible for reaching out to these contacts listed by Mat and inquiring
about willingness to help?

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Reply to this email directly or view it on GitHubhttps://github.com//issues/111#issuecomment-28193716
.

MATTHEW TODD | Senior Lecturer and Honours Coordinator
School of Chemistry | Faculty of Science

THE UNIVERSITY OF SYDNEY
Rm 519, F11 | The University of Sydney | NSW | 2006
T +61 2 9351 2180 | F +61 2 9351 3329 | M +61 415 274104
E [email protected] | W
http://sydney.edu.au/science/chemistry/research/todd.html

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This email plus any attachments to it are confidential. Any unauthorised
use is strictly prohibited. If you receive this email in error, please
delete it and any attachments.

[PatrickThomson]

I'll ask around my university about this, or in-case I need to do any separation in future.

[mattodd]

Related: #119

[mattodd]

Closing before March 2014 meeting (http://malaria.ourexperiment.org/osddmalaria_meeting_/9470) owing to shift in focus away from MMV670652 towards synthetically more tractable MMV669844