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View Full Version : Can we all put our thinking caps on and do a little talking about CFT?


Ford Prefect
2008-10-28, 08:02
"The compounds 2-carbomethoxy-3-(4-fluorophenyl)tropane and (...) are both some 60 times more potent than cocaine. These compounds could well be of interest to some clandestine chemists as taking one kilogram or cocaine and converting it into a product some sixty times more potent would obviously be quite cost effective."

Future Synthetic Drugs of Abuse
Donald A. Cooper, DEA

Most studies have shown that it's actually a little more in the 3 to 10x as potent range, but that wouldn't be the first time a DEA agent has made a mistake. One thing Mr Cooper does have correct is that it has the potential to be pretty cost effective, 'specially if you weren't to make it like he proposes.

Say we's got tropinone, which wouldn't have to be much of a stretch considering atropine can be extracted from nightshade, hydrolyzed to form tropine and oxidized to form tropinone.

With tropinone we could have 2-Carbomethoxytropinone.

"A mixture of 1.35 g of sodium methoxide (this is sodium in a minimum amount of methanol), 3.5 g of tropinone, 4 ml of dimethylcarbonate and 10 ml of toluene is refluxed for 30 min. Cool to 0°C and add 15 ml of water that contains 2.5 g of ammonium chloride. Extract the solution after shaking with four 50 ml portions of chloroform, dry, evaporate the chloroform in vacuo. Dissolve the oil residue in 100 ml of ether, wash twice with a mixture of 6 ml of saturated potassium carbonate and three ml of 3 N KOH. Dry and evaporate in vacuo to recover the unreacted tropinone. Take up the oil in a solution of aqueous ammonium chloride and extract with chloroform, dry, and evaporate in vacuo to get an oil. The oil is dissolved in hot acetone, cool, and scratch inside of flask with glass rod to precipitate 2-carbomethoxytropinone."

Yeah. (1 (http://www.erowid.org/archive/rhodium/chemistry/cocainesynth.buzz.html))


Now from 2-Carbomethoxytropinone toooo...
2-carbomethoxy-3-(4-fluorophenyl)tropane.

I'm guessing for this we'd need some Para Fluoro Benzoic Acid, which I'm also guessing we'd want to make from Para Amino Benzoic Acid. React with NaNO2 to produce the diazonium salt which is then reacted with sodium fluoroborate or fluoroboric acid very fucking carefully.

The Fluoroboric acid can be made from hydrofluoric acid & boric acid, but we wouldn't want to be using glass for that bit.



This thread is getting way too long so I'mm gonna leave it at this for now. Any ideas concerning the missing steps? Any dangerous and glaring errors I've overlooked?

-F☺rd

fcknut
2008-10-28, 09:44
Just a note, HF is not something you should be working with without training...

There's really, really, really nasty shit, then there's HF, which will eat through your skin and sequester the calcium from your bones and soft tissues, before causing you to die a very painful death...

So, it goes well beyond "not using glass for that bit" and on past ensuring you're working in a good fume hood, wearing full PPE, have access to a ventilator and ample suplies of calcium gluconate, and that you REALLY know what the fuck you're doing...


EDIT:

For the synth, I guess it depends how non- OTC you can go... (http://www.evilshare.com/64fa13ea-f676-102b-bdf3-0007e90cfb90)

From tropinone, it's probably possible to selectively enolize and alkylate at the right position to obtain an appropiately situtated presursor to the ester. Seems reasonable that a suitably bulky/chiral base would allow access to one enolate and not the other...

With that in hand, you may be able to reduce the ketone, convert to a leaving group, and knock it out with 4-fluoro-phenyl magensium bromide or some such...

Stereochemistry would be an issue for each step mind, though there's a sporting chance you might get preferential formation of the desired isomers simply throuhg substrate control.

Is there anything on the bioactivity of the corresponding diester, or alternate monoester? Or the various stereoisomers? Or perhaps the benzylic homologue - which could maybe be accessed via Wittig reaction and hydrogenation...

Hmmmm....

fcknut
2008-10-30, 18:20
I'm interested in this, purely for academic reasons as I (genuinely) would never synth anything illegal ! Too much paranoia!

But I don't have the time to read through these eight references (http://depositfiles.com/files/efr3yoe2l) just for my own gratification... Perhaps someone else will provide me with the aforementioned gratification... ;)

Have fun!

FullMetalJacket
2008-10-31, 10:06
Weird, a close friend of mine brought this up (from that reference) just the other day... placeholder post, I'm going out, will update later.

Naminator01
2008-11-03, 22:48
You don't have to use HF....

stateofhack
2008-11-04, 18:26
You don't have to use HF....

Expand please :)