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Exploration of benzylic amines #50

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david1597 opened this issue May 30, 2018 · 2 comments
Open

Exploration of benzylic amines #50

david1597 opened this issue May 30, 2018 · 2 comments
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Molecule Suggestion On Hold for projects and ideas that are currently on hold

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@david1597
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Reposting this comment from @MedChemProf as it deserves it's own issue.

While @david1597 is working out the conditions for what looks to be an efficient route to new benzylic alcohol analogs, we were interested in synthesizing the amino variant through the traditional route. To be consistent, we will also make the tertiary alcohol as a comparison:

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@david1597
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I think this is a great idea and a timely one to pursue in terms of our current priorities. I saw this paper yesterday and thought it could be a neat idea for our compounds - and then remembered @MedChemProf had already suggested exploring an amino replacement for the benzylic alcohols. We're still waiting on confirmation but the Pfizer compound currently suggest that exploring this area is not only giving us great potency but also improving parameters such as lipophilic efficiency. I feel that more resources directed in this area, at this current moment in time, is a good thing.

@mattodd
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mattodd commented May 31, 2018

Agreed. I like the idea a lot. Non-trivial chemistry, so of particular interest to the organic chemists in OSM, but absolutely a justified target based on the work of the Pfizer team, I'd say, building on top of some of the previous SAR. If no naysayers, then we can eventually close this issue and install the compound on the DCNYS page with a back-link here.

@MFernflower MFernflower added On Hold for projects and ideas that are currently on hold and removed Being Synthesised Now labels Jul 25, 2018
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