Miscellaneous

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27 Dec

Puzzled over MS

Published by KatB

Subject 

Rants, Miscellaneous

Background
Relevant experiment.  Basically, the Pictet-Spengler to form 3 PZQ analogues and PZQ itself.
The mass spec is of a by-product of the acid mediated PS cyclisation of MNR10-1 to form KAB8-1, aka the dimethoxy N-benzoyl PZQ analogue.

02 Dec

Two weeks in the PZQ lab

Published by KatB

Subject 

Rants, Miscellaneous

 
I've now reached the end of my second week in the lab working on the Pictet-Spengler route to praziquantel.
 

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

Now we're getting somewhere but not with the oxidation

Published by pylioja

Subject 

Miscellaneous

Ok now I'm getting close to TCMDC-123812/123794. A slight change of tack for the alternative core synthesis seems to have paid off. First alkylation of ethyl acetoacetate with chloroacetone and then condensation with 4-fluoroaniline appears to have given the pyrrole with an ester on the 3-position quite nicely in 61% yield over the two steps after recrystallisation (PMY 8-1). Sometimes it just pays to change the plan completely when you feel like progress is slow.

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:
 

08 Nov

Alternative Approach to the Diamine Precursor

Published by CreativeChemistry

Subject 

Miscellaneous

 We have looked at an alternative process to generate the diamine precursor to PZQ, whose resolution is documented. The process involves reduction of the cyano-imine derived from the published reaction of THIQ with peroxide/tungstate/cyanide. Having been able to reduce 1-cyanoisoquinoline very cleanly using Pd/C we anticipated that it would be possible to do the same here. It would be important, however, to maintain acidic conditions to prevent the retro-addition of the cyanide (well documented for the 1-cyano and 1-(nitromethyl)isoquinolines with a free N-H).
 

Case for characterisation of PZQAmine (or any other resolved intermediate)

Published by ndt228 on 7 November 2010 - 7:38pm

Subject 

Miscellaneous

Now that both racemic and single enantiomer PZQAmine are available, it is possible to determine phase diagrams - either binary, based on MPt, or ternary based upon solubility.  But why do this ?

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