Author Topic: prodine one step via schmidle et.al with a twist (Read 476 times)

jon · « **on:** November 11, 2009, 05:47:11 AM »

you know a-methylstryene is easy to get in 40 kg drums for 700 bucks pm for source.
well mix that with propionic acid and 1,3,5 hexahydrotrimethyltrazine reflux four hours at 140c and whalla!
25% desmethylprodine wiki it.
now incorporate 1-phenyl--3-propylamine and you get a derivative thats 21x morphine refer to:

http://www.unodc.org/unodc/en/data-and-analysis/bulletin/bulletin_1957-01-01_4_page006.html

look at entry 35 in the following chart

http://www.unodc.org/images/odccp/bulletin/bulletin_1957-01-01_4_page006_img007_large.gif

let's get this party started fellas!
pm me for the sources.

jon · « **Reply #1 on:** November 11, 2009, 06:10:42 AM »

i have a colleague who worked on this synthesis we can offer pointers
this modification would make a prodine 21 x the potency of morphine in a one pot shot let's start bubbling and stop talking my motto.
oh and don't ask stupid quests about mptp.
this has been studied mechanistically ad nuseum bioassyed and tlcs ran usin chcl3 meoh gradient and iodoplatinate as visualizing agent under uv.
guess what? nobody's got parkinsons.
so please don't waste my time.

hmm mptp rf .42 on merck silica 1/3 chcl3 meoh gradient

zzhuchila_clocker · « **Reply #2 on:** November 11, 2009, 07:05:25 PM »

what is methylene group source in one pot reaction with 3-phenyl-propylamine? paraform?

jon · « **Reply #3 on:** November 11, 2009, 08:01:07 PM »

i'll get the patents it's a mannich scheme look into schmidle and mansfield "synthesis of esters" on espacenet.com under author search and you shall find gold one pot pne step w/ this modification 20 + X morphine beautiful it does'nt get much easier than mix 3-4 chemicals and reflux.
formalin to answer you question

jon · « **Reply #4 on:** November 12, 2009, 08:48:28 PM »

here
http://v3.espacenet.com/publicationDetails/originalDocument?CC=US&NR=2765314A&KC=A&FT=D&date=19561002&DB=EPODOC&locale=en_EP
search schmidle and masfield they work on many similar compunds also hartough et. al.

zzhuchila_clocker · « **Reply #5 on:** November 21, 2009, 08:26:36 PM »

nothing is opening.. or at least i can not view it

2bfrank · « **Reply #6 on:** November 24, 2009, 12:17:59 PM »

Working this end, but Ill attach, as its something somewhat GOOD.

2bfrank · « **Reply #7 on:** November 25, 2009, 03:08:39 PM »

oops, attached the same one twice, Heres the other one out of 3 that are related btw, That last one of the 3, I did attach, shows one molecule apparently 3219 times the potency relative to Miperidiine, that could be obtained from Jons presented patent. quite an old paper too. 1962

Frank

2bfrank · « **Reply #8 on:** November 26, 2009, 02:29:56 AM »

Quote from: zz-zhuchila on November 21, 2009, 08:26:36 PM

nothing is opening.. or at least i can not view it

@ zz-zhuchila, Just so you know, the first(2) attachment I posted, was the patent Jon posted. I should of been more clear.

@ Jon, Great patent btw, very interesting molecule and the fucking ease, spun me somewhat.. I included the ones I attached, as they're somewhat related to the intermediate of the patent you presented, as well as a similiar way to obtain related molecules, but not as direct as the patent you attached..
Ive got some other stuff concerning tripeptides being bonded to some of these type of molecules that also boost bioactivity dramatically.. I dare say, this is going to be very much worked on, that is, adding various di, tri, etc, peptides to existing bioactive molecules. Ill try and hunt the paper down, as it is very interesting. Perhaps its old hat, but I hadn't seen much on this, Ill hunt the paper down some time today.

Frank

jon · « **Reply #9 on:** December 05, 2009, 02:13:19 AM »

gettin off course 2B look it's this simple mix 1phenyl-3-aminopropane (pm me for where to get) with formalin.
basify this the triazine floats to the top. sep this.
now mix with a-methylstrene, propionic acid and anhydrous h3po4 and cook.
acid base workup and vac distill, 21 X morphine one step one pot.
can't get much easier.
in fact this is the easiest opiate synthesis ever concieved if you want something easier well you shit outta luck mix 4 chemicals cook at 140 c let stand and workup shit simple and the chems are industrial and avaialable in lalrge quantitiels with out even a blink of suspiscion.
the mechanaism is double mannich acid catalysezed the second amine splits off with the help of acid the acid forms anion the benzylic carbon froms stable tertiary carbonium ion they meet up and whalla prodine compounds!!!

the rush from these kind off drugs excedd herion in euphoria too unparalled the vry best of the best fentanyl does'nt cause much euphoria but these are a different story.

hypnos · « **Reply #10 on:** December 05, 2009, 07:19:40 AM »

jon you just get better with time--i have to say thanx for all the interesting and valuable things you bring here

keep up the great work amigo

jon · « **Reply #11 on:** December 05, 2009, 11:32:45 AM »

not better with time i just got out of the psychiatric hospital so i'm thinking much more clearly (i'm severly bipolar)

2bfrank · « **Reply #12 on:** December 09, 2009, 11:35:44 PM »

Jon, as said, i included those other patents, and sorry if it has appeared, or has thrown this of course, and in hindsight i perhaps shouldn't of posted that Information, and done so elsewhere, but saw the relationships, the use of a mannich reaction as well as another prep and thought it would give more scope, more possibilities for someone who wanted to look into the chemistry of this.
I just wasn't including what I did, due to not understanding such ease. So Ill be more mindful of where i post additional information regarding a reaction or similar reactions with respect to this type of chem. So sorry to of cluttered up this thread, that clearly is about prodine via such ease. I just got somewhat excited, over enthused, and will perhaps talk to the mods and see if those posts may be better somewhere else, albeit regarding similar chem..

Hope your more settled with things, and of course, great thread, the patent you presented,and the twist, spun my head at the ease, and sorry if it has appeared that Ive jumped on it. Ill talk to the mods.

2bf

jon · « **Reply #13 on:** December 10, 2009, 12:57:59 AM »

in the patent they state other amines can be used ina similar work they used a dialkylamine and got lower yeilds due to steric factores but in this case steric factors wo'nt come into play.
on a realated note it seems feasable that this amine could easily be made by reductively aminating cinamaldehyde, cassia oil.

2bfrank · « **Reply #14 on:** December 11, 2009, 08:56:40 AM »

Yep, that would be direct rather than say using NH4Cl and getting to the 4-Phenyl-4-piperidinol and having to work that way. I have to have a better look at some of these products. Find out the effect some of these esters with other amines used, and their bioactivity etc. How would pea go with this, its one carbon short from what youve proposed. Not giving up by a long shot getting to the 1 phenyl-3- aminopropane, but just curious.

jon · « **Reply #15 on:** December 13, 2009, 02:33:08 AM »

oh the sar on the phenylethyl derivative?
it's only twice as potent you want 3 carbon separation on those phenylpiperidine analgesics.

2bfrank · « **Reply #16 on:** December 14, 2009, 03:09:56 AM »

Thanks for that clarification. Hmmm, sounds fucking nice.

jon · « **Reply #17 on:** December 16, 2009, 07:41:48 AM »

it is fucking nice you should read the reports of mppp users they describe a very euphoric rush.
dude that's the wrong patent it's us 2,765,365 not 364 go to espacenet.com
and enter that number no dashes commas or spaces.

2bfrank · « **Reply #18 on:** December 16, 2009, 10:41:19 AM »

I am confused with this Jon, as I read your earlier post in this thread re:
http://v3.espacenet.com/publicationDetails/originalDocument?CC=US&NR=2765314A&KC=A&FT=D&date=19561002&DB=EPODOC&locale=en_EP
search schmidle and masfield they work on many similar compunds also hartough et. al.

and because ZZ-zhucla couldn't open it, I saved it and posted it, and accidently posted it twice, along with a patent, that I thought was somewhat related.
The patent from that v.espacenet site brought forth a patent no US2765314, preperaton of esters, which I thought covered what this thread was about.

jon · « **Reply #19 on:** December 16, 2009, 04:38:55 PM »

this is the one
should have spelled it schmidle, mansfield, hartough et al.

Author Topic: prodine one step via schmidle et.al with a twist (Read 476 times)

jon

prodine one step via schmidle et.al with a twist

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zzhuchila_clocker

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2bfrank

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