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Author Topic: propionoxy ester of loperamide being made as we speak and tried  (Read 1682 times)

jon

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propionoxy ester of loperamide being made as we speak and tried
« on: October 11, 2009, 02:59:21 AM »
ya know swij will give full details into synthesis but he did it right this time  and damned it it does'nt have mu agonist properties it's even water soluble and loperamide s'nt so the esterification makes this compound much more user friendly so to speak.
 loperamide=immodium.
he'llbe back with the full expirimental onset is slow and you feel a warm feeling notably in the legs it's from swij's past expirience a good narcotic.

jon

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #1 on: October 11, 2009, 03:18:46 AM »
feeling noddy and pinpoint  pupils classic signs it worked no doubt.

styphnate

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #2 on: October 11, 2009, 06:00:01 AM »
Not to put too fine a point on it, but aren't you being *very* closely watched right now?  Perhaps not the best time for this.

Even still, I look forward to the write-up.

jon

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #3 on: October 11, 2009, 06:26:14 AM »
well it is'nt all  that great anyway definetly different but it's sort of weak not really worth the effort.
besides loperamide is'nt illegal.

styphnate

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #4 on: October 11, 2009, 06:31:43 AM »
Good point, but I tend to think it wouldn't help your case.  Though maybe I'm wrong, as I suppose it could serve as evidence of legitimate laboratory research. ::)

Vesp

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #5 on: October 11, 2009, 06:41:24 AM »
Has anyone tried loperamide with Quinidine? Might help out here as well...
Has the acetoxy, or others been tried?

Quinidine probably isn't super easy to get, but perhaps it can be made some how from quinine?
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jon

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #6 on: October 11, 2009, 09:55:57 AM »
mannitol seems to work with loperamide alone i can only imagine how much better this woud be.
your's truly tried it with mannitol alone thinking it was b.s. lo and behold it was quite dreamey but the brain figures out how to bring that fun to and end somehow.
biology sucks!
« Last Edit: October 11, 2009, 09:57:39 AM by jon »

hypnos

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #7 on: October 12, 2009, 04:02:48 AM »
yeah it can give you the shits!!!!!!!!

is that why the loperamide ;D ;D
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Fra

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #8 on: October 13, 2009, 04:13:10 PM »
I'm interested... would you mind to reporting the experience? and please, post the synthesis. anyhow, I wonder how much you spent: imodium and generics aren't cheap, and they contain few mgs.

jon

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #9 on: October 14, 2009, 07:33:10 AM »
not worth the trouble mild opiate effects it's detrius unless you can pluck that chlorine atome of the benzene ring (not easy to do)
 big pharma has it licked.

jon

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #10 on: October 14, 2009, 04:51:54 PM »
btw the way think costco

ergoamide

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #11 on: October 23, 2009, 09:45:53 AM »
If it is use intravenously then it's effects ra every nice and strong aswell, about as strong as heroin although the high isn't quite as good as heroin but what is?

no1uno

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #12 on: October 23, 2009, 06:38:38 PM »
Maybe try oxidizing that 4-hydroxy to a ketone and putting aniline on it?

Should markedly alter the pharmacology - especially if you then make the N-propionate of that sucker
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no1uno

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #13 on: October 24, 2009, 05:28:47 AM »
I mean, contrary to what has been written elsewhere, it should be absolutely fucking impossible to, without drastic fission, make MPTP/MPP+ analogues from this - the construction of the quaternary bond between the piperidine and the phenyl is already completed (and that is where the fuckup lay).

But if the propionic acid ester of that tertiary alcohol is not active enough, then it is highly likely that the fentanyl analogue will be (there are fentanyls which have a quat configuration at that 4-piperidine, from memory there is a methyl? A p-chlorobenzene might be too bulky, but hell, who knows?). Also note, there are PCP analogues (ie. very fucking similar if a cyclohexyl group were added in), modified on the benzene ring, that reportedly have high affinity (some 430 times higher than PCP) for the morphine receptors.

In terms of structure relationship shite, this could be fucking interesting

{edit}

Away with the fucking fairies - ain't no way we can oxidise that fucking thing, it will have to be transformed to the halide then displacement of that by the aniline, what is going to do that job?

Or even more to the point - is the molecule going to survive this (nb. hitting that hydroxyl with propionitrile, then forming aniline from that with NaH and more to the point, is it really worth knowing)?
« Last Edit: October 24, 2009, 11:39:37 AM by no1uno »
"...     "A little learning is a dang'rous thing;
    Drink deep, or taste not the Pierian spring:
    There shallow draughts intoxicate the brain,
    And drinking largely sobers us again.
..."

jon

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #14 on: October 31, 2009, 04:30:45 AM »
in response to
Has the acetoxy, or others been tried?

yes, it's nowhere near as good as the propionoxy ester ya know loperamide is'nt water soluble  but it's ester is,  so injection of this should be tried next expiriment.

jon

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #15 on: October 31, 2009, 04:37:18 AM »
Maybe try oxidizing that 4-hydroxy to a ketone and putting aniline on it?

how you going to do that it's tertiary????

no1uno

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #16 on: October 31, 2009, 05:02:36 AM »
Quote from: jon on October 31, 2009, 04:37:18 AM
Maybe try oxidizing that 4-hydroxy to a ketone and putting aniline on it?

how you going to do that it's tertiary????


Thus this statement:

Quote
Away with the fucking fairies - ain't no way we can oxidise that fucking thing, it will have to be transformed to the halide then displacement of that by the aniline, what is going to do that job?[/url]

Comes from posting before looking hard enough at what I am thinking about:P
"...     "A little learning is a dang'rous thing;
    Drink deep, or taste not the Pierian spring:
    There shallow draughts intoxicate the brain,
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..."

jon

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #17 on: October 31, 2009, 05:23:32 AM »
you're alright in my book if we went head to head intellectually speaking you'd probably work circles around me, i'm not one upping you.

jon

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #18 on: November 02, 2009, 05:32:53 PM »
you know ergoamide has a point i.v. may be the ticket.
here's the logic research has concluded that it's dimethylamido moiety is n,n-demethylated hepatically 99% first pass so this explains it's mild activity on insulflattion.
bypassing first pass metabolism rectifies the situation so at least one would recieve some benefit from having thier rectum plugged up for a while.
also using hepatic enzyme inhibitors such as cimetidine would probably hinder said n,n demethylation so some actives would reach the sweet spot, synthesis shall be posted.

jon

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Re: propionoxy ester of loperamide being made as we speak and tried
« Reply #19 on: November 02, 2009, 07:44:36 PM »
the gist is this and remember think costco.com
and no it is'nt a source because it's perfectly legal to do.
remove the outer coating of the pills in a colander by rinsing with water dry on paper towel.
grind up and boil in either xylene or ethylacetate to remove carnuba wax do this twice.
common sense filter between steps.
make sure it's completely dry so one does'nt coextract carnuba wax.
now extract with hot methanol three times.
evap methanol.
should be pure enough for every gram 10 cc propionic anhydride 3 hours 100 c standard for tert alcohols.
trace h2so4 or naacetate could be employed as catalyst.
ie. 1 drop h2so4 per 10 cc or .5 gram naacetate ala ziering et. al.
swij never does this as practice but has before and he does'nt have parkinson's.
easiest way to work up rotovap or evap anhydride on pyrex dish with blow dryer, rinse with acetone.
or you could get tedious and add water freebase and extract into chloroform evap, etc.
not nessecary though.


side note it does'nt all dissove in the anhydride don't worry about it if your concerned a higher boiling chlorinated solvent will dissolve loperamide and remain inert to propionic anhydride.



*But if the propionic acid ester of that tertiary alcohol is not active enough, then it is highly likely that the fentanyl analogue will be (there are fentanyls which have a quat configuration at that 4-piperidine, from memory there is a methyl? A p-chlorobenzene might be too bulky, but hell, who knows?). Also note, there are PCP analogues (ie. very fucking similar if a cyclohexyl group were added in), modified on the benzene ring, that reportedly have high affinity (some 430 times higher than PCP) for the morphine receptors*
this statement is very interesting, any references?
« Last Edit: November 02, 2009, 07:50:46 PM by jon »
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