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Stimulants of the Future II

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count the carbons.... this needs special chemistry, or special chemists or chemists who are special
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All you would need to do would be to replace the amine with a 1-methyl-pyrrolidin-2-yl moiety, and this should be doable in 2 or 3 steps I think.

However I'm no expert and I might be mistaken. I probably am, I do that a lot.

If so forget everything I've said. Except for the molecule being a nice DRI.
 
All you would need to do would be to replace the amine with a 1-methyl-pyrrolidin-2-yl moiety, and this should be doable in 2 or 3 steps I think.
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Without going into synthesis details, what you're proposing is going to be a pain in the arse and propably result in tiny yeilds


I want absolutely zero opioid effects from stimulants. The idea stim for me would be MDPV with some GABA mixed in.

Either that or for productivity and physical transparency propyl-amphetamine can't be beat.
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But the slight opioid activity reduces the obsessive, thought loop type side effects that can really bugger the focus required for productive activity (as opposed to looking for things on the floor that don't exist for hours on end =D)
 
as opposed to looking for things on the floor that don't exist for hours on end
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Argh, don't get me started! I've often been ultra-frustrated at tweakers who spend hours crawling on the floor searching for non-existant drugs!
 
fastandbulbous said:
as opposed to looking for things on the floor that don't exist for hours on end =D
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whatever you do, do NOT take off your shirt in your house and misplace it somewhere. Oh you should know the feeling racing around for 2.5 hours trying to find it. Not that I even care about that shirt, but the challenge of searching for it is unrepressible.

BTW phenylephrine > 3-chloro aminorex looks very possible. The 3-chloro (on the benzene ring) will surely diminish function of the aminorex but should still be active, halogen is in the same position as in bupropion (and bupropion is weak for other reasons- the ketone, the tert-butyl does god knows what). Except it's possible the ephedrine > 4-MAR synthesis would be screwed up on this.
 
I wonder what exactly effects a-keto phenethylamine would have. Phenethylamine would be really active (right?) if it didn't get devoured by MAO which goes something like this:
GabeTheNerd_01_in_2008.png

Now if you had a ketone in the R-a position what would happen? MAO couldn't seriously oxidize it to CO2 + ethylbenzene, right?
 
chloral hydrate said:
Oxycodone like all of those morphine derivates are dopamine agonists as well as opiod agonists. D1/D4 dopamine agonists have some stimulant effects, D2/D3 agonists just make people spew.

""D1-selective full agonists like SKF-81297 and 6-Br-APB produce characteristic anorectic effects, hyperactivity and self-administration in animals, with a similar but not identical profile to that of dopaminergic stimulants such as amphetamine""
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That explains why the mu opioid agonist effects of hydrocodone are hardly noticed by me...
 
^I agree coolio. It seems to me like vicodin has a much more dopaminergic feel while not as noticeable opioid feel compared to something like codeine.

You know bulbous if it does work, I doubt there will be crowds of people since you'd need at least two particular reagents which require a bit of work to make, but at least we could do something with all this phenylephrine the DEA's been handing us!

So that's a "no" on the benzenamide dread? I didn't really think it stood a chance.
 
I'm wondering why Fencamfamine has any opioid activity at all.No quartenary C etc.
Maybe one should do the 3-Methoxianalog?

And I can imagine the bicyclus arranged so that a quartenary carbon results on the benzylic position.
 
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negrogesic said:
And of course a 3'4' methylendioxyaminorex product could potentially be made using phenylephrine....
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It can't be that simple, can it? Now say if you have some 3,4-dichloro analogue than everything you need to make a 3,4-methylenedioxy you probably already have at home. But just a 3-position?

dread said:
It would very probably metabolize very rapidly into phenylacetic acid. Which I believe is inactive.
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Yeah the hydrochloride salt hydrolyzes apparently to phenylacetic acid, so it's useless. But still I bet there can be new innovative ways of inhibiting MAO oxidation besides an a-methyl group or an aminorex-type thing.

Fencamfamine is interesting, the nitrogen is too close for it to have a morphine like backbone, but then again perhaps the fact that one of those rings is "norbornane" means there's three rings in that one ring. Whether or not it has that high opiate binding, I've heard it's pleasant. They should make some analogues.
 
hugo24 said:
I'm wondering why Fencamfamine has any opioid activity at all.No quartenary C etc.
Maybe one should do the 3-Methoxianalog?

And I can imagine the bicyclus arranged so that a quartenary carbon results on the benzylic position.
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4-methoxy is probably the way to go, actually. Somewhere, I think blacklight, I have a chart that looks at those opioids for which 3-methoxy is better and those for which 4-methoxy is better, and based on the similar structural similarities, this would fall into the latter category.

Should be fitting the same place that the tyrosine residue of the peptide agonists
 
Phenylephrine could be made into
N-methyl-beta-methoxy-3-methoxyphenethylamine.
 
Hammilton said:
4-methoxy is probably the way to go, actually. Somewhere, I think blacklight, I have a chart that looks at those opioids for which 3-methoxy is better and those for which 4-methoxy is better, and based on the similar structural similarities, this would fall into the latter category.

Should be fitting the same place that the tyrosine residue of the peptide agonists
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For those of us who aren't members of blacklight, any chance you could put that table ip of the 3-methoxy vs 4-methoxy sub? 3-methoxy does seem to feel to be the right position to try first with any compound you want to boost the opioid activity of - from what I've read of 4-methoxyPCP & sampled of 3-methoxyPCP, I'd say the winner in that case is the 3-methoxyPCP - an extraordinarily stress free dissociative IMO
 
Maybe it has something to do with the number of carbons between the phenyl and the amine.

PcP: 1 carbon - 3-methoxy
Fencamfamine: 2 carbons - 4-methoxy
Pethidines, morphines etc: 3 carbons - 3-methoxy

so I extrapolate from this: even number of carbons = 4meo, odd number = 3meo.

It probably isn't that simple, but I like playing with thoughts for fun.
 
You can't consider morphines here, since depending on how you count, you can get 2 or 3 carbons. There are a lot of others that could be included, but the results are about the same.

meta_or_para.gif
 
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You can't consider morphines here, since depending on how you count, you can get 2 or 3 carbons.
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Good point. On the other hand, if you count the 2-carbon way, then the hydroxy group seems to be in the 4-position!
 
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