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OpenSourceTB / OSTB_Series4_OpenCyclams

The fourth OSTB series, based on a set of functionalised open-chain polyamines.
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Tetrapendant compounds #2

Open MFernflower opened 3 years ago

MFernflower commented 3 years ago

These should be easy to make as the tetrapropargyl precursor could likely be made in a solvent-less fashion: CORE111

tetrapendant

MFernflower commented 2 years ago

@KlementineJBS Is something like this being considered for synthesis?

KlementineJBS commented 2 years ago

Yes, we are considering this kind of thing - though currently still working on trying to do the boc-protected bis- versions.

Another researcher successfully made a tetrapendant compound from a 1,8-diaminooctane scaffold, but found it had a >100 micromolar MIC against the H37Rv Mtb strain. Unfortunately most of my own lab work has ground to a halt due to severe covid-19 restrictions, so it may take some time until we can get onto making this kind of compound ourselves on different scaffolds...

Also, when you say it can be made in a solvent-less fashion - could you explain what you mean? I haven't seen that kind of scheme before.

MFernflower commented 2 years ago

@KlementineJBS I was assuming that at a small scale the tetra-propargyl precursor compound (to the feed into the click rxn) could be made in solvent less fashion as the reagents to make it are liquids (propargyl bromide and the diamine)

KlementineJBS commented 2 years ago

Oh! I get what you mean now and that makes a lot of sense - I've been struggling over what solvent to use so definitely will consider giving this a go when I can get back in the lab.