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Stimulants of the Future II

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As far as I know, it is that polar -OH that stops ephedrine from crossing readily, it is speculated that if it did cross it would be very similar in effects to its 'cousins'

To continue my point, look: 2-benzylpiperidine crosses (analogous to methamphetamine), but with an -OH it is ritalinic acid (analogous to ephedrine) and doesn't cross, but with a reverse acetate ester it is phacetoperane (analogous to methylamphenidate) which does cross.

As such I think that "methylamphenidate" will cross and should be quite active. Furthermore if I'm correct with that acetic anhydride stuff, it should be extremely easy to make.
 
As far as I know, it is that polar -OH that stops ephedrine from crossing readily, it is speculated that if it did cross it would be very similar in effects to its 'cousins'

To continue my point, look: 2-benzylpiperidine crosses (analogous to methamphetamine), but with an -OH it is ritalinic acid (analogous to ephedrine) and doesn't cross, but with a reverse acetate ester it is phacetoperane (analogous to methylamphenidate) which does cross.

As such I think that "methylamphenidate" will cross and should be quite active. Furthermore if I'm correct with that acetic anhydride stuff, it should be extremely easy to make.



Yes it works, but with acetic anhydride you also end up acylating the piperidine nitrogen (anyway, less synthetic discussion please)
 
As far as I know, it is that polar -OH that stops ephedrine from crossing readily, it is speculated that if it did cross it would be very similar in effects to its 'cousins'

To continue my point, look: 2-benzylpiperidine crosses (analogous to methamphetamine), but with an -OH it is ritalinic acid (analogous to ephedrine) and doesn't cross, but with a reverse acetate ester it is phacetoperane (analogous to methylamphenidate) which does cross.

As such I think that "methylamphenidate" will cross and should be quite active. Furthermore if I'm correct with that acetic anhydride stuff, it should be extremely easy to make.



well I know they use AA to make heroin cross the BBB faster than morphine. Don't know how compatible it would be with methamphetamine.
 
Since "chloral hydrate" posted another methylphenidate like compound please think again about my "(Methyl-)Amphenidate" idea:


methyl%203-hydrazinyl-2-phenylbutanoate55.png



The idea behind it was the following:

Since Methylamphetamine is primary a dopamine releaser and Methylphenidate a dopamine reuptake inhibitor I thought why not try to combine both mode of actions together in a single molecule? I think it was at least worth a try.

@Hammilton: Although I really value your knowledge - I have to please you not to get impolite again only because you disagree with a idea or the fact that someone can't explain the pharmacological background of a thought as well as you. Thanks.
 
I really like that amphenidate idea/ methylamphenidate. Obviously, the methyl acetate makes a large difference to 2-benzyl piperidine, which is only a strong norepinephrine reuptake inhibitor. As such one can only guess what effects amphenidate would have.

Except that -HN-NH2 in your drawing is supposed to be -HN-CH3, right?
 
Methamphenidate sounds more street cred than calling it "methylamphenidate"

Woah, I overlooked the fact that the structure drawn is a hydrazine. That's probably gross toxicity.

See for procarbazine.

"It is also highly carcinogenic—patients have a 5–10% risk of developing acute leukemia...

and is generally priced at $50/capsule in the United States.[1]"
 
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ephedrine does come from plants, but as far as I'm aware, most ephedrine used in methamphetamine synthesis is produced synthetically, and amphetamine obviously is.

ham
 
Right, although it would be pretty convenient to grow a shrub of ephedra I suppose... it has an ephedrine content of 2.2% so a 1kg shrub add HCl you'll probably get at least 100g ephedrine.
 
Benzaldehyde is found in almond oil.

Also, amphetamine could be easily synthesized from extracted cathinone found in the African plant known as khat.
 
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Imitation almond flavoring is 15-20% benzaldehyde I believe.

Sure, ethanol + HCl + Zn = ethyl chloride, pour that over Khat and you got diethylcathinone... and Khat is psychoactive in itself...nice.
 
Dextro-amphetamine sulphate (or hcl) from raw khat plant material would be uber nice.

They might even set up factories in the African jungle.

(Dextro b/c khat being a plant makes only one isomer of cathinone--the S)
 
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No, you wouldn't.

Either the Clemmenson reduction (Zn(Hg), HCl) or the Wolff Kishner (NH2-NH2, KOH)--I forget which; one is for basic conditions, the other for acidic ones--would take the ketone off in one step and probably many other reactions that I don't know about as well.

You could reduce the ketone and go through the cathine as well, but that would be two steps. Anyway, no synthesis discussion.
 
Was looking around, found something about 1-methyl,4,4-diphenylpiperidine

4,4-Diarylpiperidine compounds, preferably 4,4-diphenylpiperidine which are
substituted or unsubstituted in the 1-position of the piperidine nucleus, such
as 1-(lower alkyl)-4,4-diphenylpiperidines, 1-(lower alkyl)-4-phenyl-4-tolyl-
piperidines, and their substantially non-toxic, pharmaceutically-acceptable acid
addition salts, are highly effective central nervous system (CNS) stimulants
which are superior to known amphetamine-type stimulants."
 
Right, although it would be pretty convenient to grow a shrub of ephedra I suppose... it has an ephedrine content of 2.2% so a 1kg shrub add HCl you'll probably get at least 100g ephedrine.

Is 2.2% for dried plant or including moisture?

100g = 10g presumably?
 
Dextro-amphetamine sulphate (or hcl) from raw khat plant material would be uber nice.

They might even set up factories in the African jungle.

(Dextro b/c khat being a plant makes only one isomer of cathinone--the S)

Fucken-A. I didnt know that (seriously). It's just not something I had thought about before.
 
Do you know about budipine yet? I only saw it the other day personally.

Oh yep, that's it. So it does not seem to be that impressive, yeah? Seems more like a dopaminergic agonist than a stimulant.

And yeah that was supposed to be 10g, which I guess is only about 20 boxes of 50*10mg pseudoephedrines.

Khat seems wonderful, I wonder what the alkaloid content of it is...
 
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