3-(dimethylamino)-2,2-dimethyl-1-phenylpropan-1-one

[Fertile]

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As strong as demerol, 1 step from 2 common precursors.

 

[Fertile]

Note similarity to:

n hosted at ImgBB

Image n hosted in ImgBB

ibb.co

Although the latter has a chiral amine and no paper resolves them.

This work is also covered by CA Patent 830475A 'Analgesic cyclobutanes derivative compositions'

What is interesting is that this class is similar to Lednicer's (much more potent) BDPC (and homologues). The above has more rotatable bonds and is not the ideal biosteric minimum. I have no idea if adding a p-Br to the benzylamine would increase affinity, but it seems quite likely. With this class, if one can obtain the precursor, it is synthetically simple.

There are many workers who had limited funding for the research of opioids. Until the 1970s nobody really understood what requirements a mu agonist required, but now there are papers with training-sets & 3D QSAR.

 

[Fertile]

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This is a homologue of ciramadol. Ciramadol is a mixed agonist-antagonist but replacing the m-OH for a p-Cl is mentioned in Reaxys as a full agonist.

 

[Fertile]

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Note similarity to second compound it list.

fastandbulbous - treat these as LEAD compounds.

 

[Fertile]

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Now, given the number of patents referencing this scaffold. Certainly the above is considered to be many times M in potency. I would have to go through hundreds of patents, but the N-methyl was in the region of M. Also the class is closely related to NMDA antagonists. Specifically 8A-PDHQ.

 

[Nurse Ratched]

The laymen that post here aren't going to understand any of this. You and fastandbulbous do this in Neuro.

Going to move the thread.

I'm sure you know by reading the first 4 pages of this sub forum , and the questions that are asked, this thread is way beyond their comprehension.

 

[Fertile]

The laymen that post here aren't going to understand any of this. You and fastandbulbous do this in Neuro.

Going to move the thread.

I'm sure you know by reading the first 4 pages of this sub forum , and the questions that are asked, this thread is way beyond their comprehension.

Well fine - but it isn't to do with synthesis - it's purely a simple pattern-matching. But as you see fit.

 

[Nurse Ratched]

Well fine - but it isn't to do with synthesis - it's purely a simple pattern-matching. But as you see fit.

Didn't say it had to do with synthesis. The thread won't be comprehended in BDD and I think you know that.

 

[Fertile]

BTW as regards to 3-(dimethylamino)-2,2-dimethyl-1-phenylpropan-1-one itself, well he makers of the propanamide substituted the dimethyl side-chains also produced the cyclobutyl which was just as active. Look at sibutramine. The bond-angle is preserved so people are free to add an alpha cyclobutyl to all of the DAT/NET/SERT PEAS.

I have no idea if this would work with the 5HT2b ligands.... still, it blows the laes on PEAs wide open.

 

[Fertile]

Didn't say it had to do with synthesis. The thread won't be comprehended in BDD and I think you know that.

People can ask - I LIKE people to ask. That's how education works. I've posted 1001 novel compounds and in 99% of cases, people ask, get an explaination and move on. The few who still struggle, I go to greater depths with reference.

It's all over the site - I don't do it as a one-off. Once people know of Chemdraw, Pubchem, RO5 and other free assets, it's not actually hard. OK we get the 1% who glory in not using assets and claiming it as some kind of victory - but those people tend to resort to swearing.... as they did yesterrday.

 

[Nurse Ratched]

People can ask - I LIKE people to ask. That's how education works. I've posted 1001 novel compounds and in 99% of cases, people ask, get an explaination and move on. The few who still struggle, I go to greater depths with reference.

It's all over the site - I don't do it as a one-off. Once people know of Chemdraw, Pubchem, RO5 and other free assets, it's not actually hard. OK we get the 1% who glory in not using assets and claiming it as some kind of victory - but those people tend to resort to swearing.... as they did yesterrday.

I get it. I hear ya. You like to post a lot. That's fine. I know you are educating people. But threads belong in certain sub forums so just go with the flow.

 

[Fertile]

If it was all correct - I would have nothing to post.

Believe me, i like being the dumbest one in the room so I can learn the most.

Put on your dunce's caps. Those caught not wearing their dunce's caps
may be forced to stand at the front and teach.
-S. Munnery

 

[Fertile]

Not moved, per se

 

[Fertile]

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Now as I said - other, related compounds have sported a cyclobutyl in place of a dimethyl but since NOBODY looked into this scaffold, who knows.

I cannot help but think that an ethylaryl in the right spot would work wonders. The dimethyl isn't required, a monomethyl is BUT then the whole thing gets chiral.

 

[Xorkoth]

I agree with Nurse. BDD is the forum for asking "HoW Do I SmOkE MeTH" or "Is this mark on m arm an abscess?". This is definitely suited for NP&D. And I hope you get some replies, because I am very curious, though sadly this is above my head in terms of being able to contribute.

I wish we had the crowd here that we did back in the pre-2010s, you'd have plenty of educated replies.

 

[Delmonte421]

Note similarity to:

n hosted at ImgBB

Image n hosted in ImgBB

ibb.co

Although the latter has a chiral amine and no paper resolves them.

This work is also covered by CA Patent 830475A 'Analgesic cyclobutanes derivative compositions'

What is interesting is that this class is similar to Lednicer's (much more potent) BDPC (and homologues). The above has more rotatable bonds and is not the ideal biosteric minimum. I have no idea if adding a p-Br to the benzylamine would increase affinity, but it seems quite likely. With this class, if one can obtain the precursor, it is synthetically simple.

There are many workers who had limited funding for the research of opioids. Until the 1970s nobody really understood what requirements a mu agonist required, but now there are papers with training-sets & 3D QSAR.

im in the process of working with some post-docs on small molecules and getting them to have higher binding affinity, well I am producing and making while they are doing the real research and telling me what reactions to do etc

 

[Skorpio]

im in the process of working with some post-docs on small molecules and getting them to have higher binding affinity, well I am producing and making while they are doing the real research and telling me what reactions to do etc

You in a med chem program? I'm more in the life sciences arena and often romanticize organic chemists, sometimes I wish I went that route (though I love having shirts without acid holes in them).