Author Topic: codeine to morphine to whatever the fuck derivative  (Read 319 times)

tryl

  • Pupae
  • **
  • Posts: 89
codeine to morphine to whatever the fuck derivative
« on: December 06, 2011, 10:00:24 AM »
i wonder, has anyone attempted the codeine to morphine CHCl3/BBr3 conversion?

seems to yield a good 80-90%, and despite being toxic as fuck, it is a rather simple procedure.

i get 200mg of codeine for a buck around here, and if this is as promising as it sounds... well, fuck me!

so, any of you opie aficionados like to throw in your 2 cents? jon? and whatever happened to jboogie, if i may inquire?
"In the words of Archimedes, give me a lever long enough and a place to rest it... or I shall kill one hostage every hour."

smellslikeindole

  • Larvae
  • *
  • Posts: 10
Re: codeine to morphine to whatever the fuck derivative
« Reply #1 on: December 07, 2011, 01:56:37 AM »
Here is a patent about this:

DR PHARMA NOVA, LLC
Patent:   WO2006/91885 A2, 2006 ;
Location in patent: Page/Page column 51-52 ;

Single 2H labeled morphine can be prepared using a modification of the procedure described in Journal of Medicinal Chemistry, 1977, vol 20, 164-165. A solution of 2.99 g (10 mmol) of anyhydrous D2-Codiene O-3 in 25 ml of CHCh is to be added during 2 min to a well-stirred solution of 15 g (59.9 mmol) of BBn in 175 ml of CHC13 maintained in the range 23-26 degrees C. A 10 ml portion of CHCh, which is added to rinse the addition funnel, is added to the reaction mixture and stirring is continued for 15 min at 23-26 degrees C. The reaction mixture which will consist of a suspension of white solid (in CHCh) is then poured into a well-stirred mixture of 80 g EPO <DP n="53"/>of ice and 20 ml of concentrated (28-30percent NHs) NBUOH. The two-phase system is kept at -5 to 0 degrees C for 0.5 h (continuous stirring) and filtered. The resulting crystalline material is washed thoroughly with small portions of cold CHCIa and H2O and dried to give 2.67 g (88.1 percent) of slightly off-white MO-3 monohydrate.

The problem is: the boron-tribromide is a really agressive chemical, not so good for a chemist without protective clothing, it can easily form a lot bad things with the skin...

The good point is: the yields are good.

Another thing is: pyridine.HCl could be also used for demethylation of codeine ad the following paper describes it:
hxxp://pubs.acs.org/doi/abs/10.1021/ja01124a538

I couldn't get this paper, just another one:

P.S. and just an idea: use the word "fuck" not so often.

RoidRage

  • Dominant Queen
  • ****
  • Posts: 386
Re: codeine to morphine to whatever the fuck derivative
« Reply #2 on: December 07, 2011, 03:36:14 AM »

Another thing is: pyridine.HCl could be also used for demethylation of codeine ad the following paper describes it:
hxxp://pubs.acs.org/doi/abs/10.1021/ja01124a538

I couldn't get this paper, just another one:


Here you go  :)

The Synthesis Of Morphine
Marshall Gates, Gilg Tschudi
J. Am. Chem. Soc., 1952, 74 (4), pp 1109–1110
DOI: 10.1021/ja01124a538

lugh

  • Global Moderator
  • Foundress Queen
  • *****
  • Posts: 876
Re: codeine to morphine to whatever the fuck derivative
« Reply #3 on: December 07, 2011, 04:00:58 AM »
Dovalatov's last words in the Bee Song:

http://127.0.0.1/talk/index.php/topic,479.msg20308.html#msg20308

are still the simple truth:

http://127.0.0.1/talk/index.php/topic,2495

Use the fucking search engine !!!
This means you !!!


 8)
« Last Edit: December 07, 2011, 04:43:45 AM by lugh »
Chemistry is our Covalent Bond

tryl

  • Pupae
  • **
  • Posts: 89
Re: codeine to morphine to whatever the fuck derivative
« Reply #4 on: December 07, 2011, 09:01:12 AM »
Use the fucking search engine !!!
This means you !!!


oh, i can well google-fu my way around.

but was just curious to hear what you, and not google, have to say.
cos this is a relatively simple conversion, with very good yields, yet i haven't heard of anyone doing it so was wondering if there is any reason behind it (beside the tribromide).
"In the words of Archimedes, give me a lever long enough and a place to rest it... or I shall kill one hostage every hour."

lugh

  • Global Moderator
  • Foundress Queen
  • *****
  • Posts: 876
Re: codeine to morphine to whatever the fuck derivative
« Reply #5 on: December 07, 2011, 06:39:14 PM »
Quote
oh, i can well google-fu my way around.

The fact that you started this thread when there was another one on the same topic a few months ago shows a deficiency in your search skills whether you want to admit or not  ::)  Please read the rules again:

http://127.0.0.1/talk/index.php/topic,369.msg12503.html#msg12503

 8)
Chemistry is our Covalent Bond

tryl

  • Pupae
  • **
  • Posts: 89
Re: codeine to morphine to whatever the fuck derivative
« Reply #6 on: December 07, 2011, 08:11:44 PM »
i think you are more mistaken than i am.

try and search for it yourself, using this forum's search.
see what ya get.

i am not disputing the fact that i might sometimes be a moron, but i hate being treated as such for no actual reason.
i mean, it is fucking obvious i know how to use a computer, isn't it?
« Last Edit: December 07, 2011, 08:15:17 PM by tryl »
"In the words of Archimedes, give me a lever long enough and a place to rest it... or I shall kill one hostage every hour."

atara

  • Dominant Queen
  • ****
  • Posts: 256
Re: codeine to morphine to whatever the fuck derivative
« Reply #7 on: December 07, 2011, 10:49:58 PM »
if you have BBr3, use it. it doesn't get written about for a reason tho.

tryl

  • Pupae
  • **
  • Posts: 89
Re: codeine to morphine to whatever the fuck derivative
« Reply #8 on: December 08, 2011, 04:16:53 PM »
what?!
"In the words of Archimedes, give me a lever long enough and a place to rest it... or I shall kill one hostage every hour."

tryl

  • Pupae
  • **
  • Posts: 89
Re: codeine to morphine to whatever the fuck derivative
« Reply #9 on: December 08, 2011, 08:24:27 PM »
yea, i eventually figured you were talking about "krokodil", and i have been meaning to try this out soon as i get the keys to the basement where my mom has locked all my glassware, RP and I.

i suppose utilizing this route you get a mixture of active and inactive byproducts, among which desomorphine.

wonder what's big deal with this, can't be too much of a hassle to purify... why are the russian junkies dropping like flies simply because they miss on one or two workup steps in the end?
"In the words of Archimedes, give me a lever long enough and a place to rest it... or I shall kill one hostage every hour."

lugh

  • Global Moderator
  • Foundress Queen
  • *****
  • Posts: 876
Re: codeine to morphine to whatever the fuck derivative
« Reply #10 on: December 08, 2011, 10:02:14 PM »
Quote
why are the russian junkies dropping like flies simply because they miss on one or two workup steps in the end?

The average lifespan of a junkie is short no matter where they're from  ::)  Improper purification techniques simply exacerbates this deadly habit  8)
Chemistry is our Covalent Bond

POSEIDON

  • Subordinate Wasp
  • ***
  • Posts: 116
Re: codeine to morphine to whatever the fuck derivative
« Reply #11 on: December 09, 2011, 04:15:48 AM »
Look this pdf
The chemists are a strange class of mortals, impelled by an almost insane impulse to seek their pleasures amid smoke and vapour, soot and flame, poisons and poverty; yet among all these evils I seem to live so sweetly that may I die if I were to change places with the Persian king.
— Johann Joachim

tryl

  • Pupae
  • **
  • Posts: 89
Re: codeine to morphine to whatever the fuck derivative
« Reply #12 on: December 09, 2011, 10:12:02 AM »
nah, junkies don't necessarily have a short lifespan.
i've met folks in their 60's that have been addicts all their lives.
i've made it through some 7-8 years, at least 5 of which as a full-blown addict.

tnx POSEIDON, i have it though. :)

as i said, i was just curious if anyone has done it, and if not, why.
"In the words of Archimedes, give me a lever long enough and a place to rest it... or I shall kill one hostage every hour."

lugh

  • Global Moderator
  • Foundress Queen
  • *****
  • Posts: 876
Re: codeine to morphine to whatever the fuck derivative
« Reply #13 on: December 09, 2011, 04:04:14 PM »
Quote
wonder what's big deal with this, can't be too much of a hassle to purify... why are the russian junkies dropping like flies simply because they miss on one or two workup steps in the end?

Quote
nah, junkies don't necessarily have a short lifespan.

The life span of a fly is rather short, so which statement is more correct ?  Are junkies in Russia dying en masse or are they living a normal life span ? Generally speaking, junkies don't last long anywhere  8)
Chemistry is our Covalent Bond

lugh

  • Global Moderator
  • Foundress Queen
  • *****
  • Posts: 876
Re: codeine to morphine to whatever the fuck derivative
« Reply #14 on: January 20, 2012, 10:39:11 PM »
Quote
whatever happened to jboogie, if i may inquire?

He's been offline, not that it's really any of your business  :-X  He wants everyone to know he's okay  8)
Chemistry is our Covalent Bond

therepublicanpartier

  • Larvae
  • *
  • Posts: 13
Re: codeine to morphine to whatever the fuck derivative
« Reply #15 on: January 23, 2012, 10:29:17 PM »
I can see where, for kitchen cooks, purifying a 1 gram batch of desomorphine while staving off withdrawl is probably not always going to happen.  But If it were possible to do an easy purification that would yield a cleaner product for smoking or insufflation instead of injection.  And by planning ahead for a larger batch, maybe some of the negative effects of krokodil could be mitigated.  It is a really simple synth.

http://www.independent.co.uk/news/world/europe/krokodil-the-drug-that-eats-junkies-2300787.html


Quote
Krokodil: The drug that eats junkies

A home-made heroin substitute is having a horrific effect on thousands of Russia's drug addicts

Oleg glances furtively around him and, confident that nobody is watching, slips inside the entrance to a decaying Soviet-era block of flats, where Sasha is waiting for him. Ensconced in the dingy kitchen of one of the apartments, they empty the contents of a blue carrier bag that Oleg has brought with him – painkillers, iodine, lighter fluid, industrial cleaning oil, and an array of vials, syringes, and cooking implements.
 

Half an hour later, after much boiling, distilling, mixing and shaking, what remains is a caramel-coloured gunge held in the end of a syringe, and the acrid smell of burnt iodine in the air. Sasha fixes a dirty needle to the syringe and looks for a vein in his bruised forearm. After some time, he finds a suitable place, and hands the syringe to Oleg, telling him to inject the fluid. He closes his eyes, and takes the hit.

Russia has more heroin users than any other country in the world – up to two million, according to unofficial estimates. For most, their lot is a life of crime, stints in prison, probable contraction of HIV and hepatitis C, and an early death. As efforts to stem the flow of Afghan heroin into Russia bring some limited success, and the street price of the drug goes up, for those addicts who can't afford their next hit, an even more terrifying spectre has raised its head.

The home-made drug that Oleg and Sasha inject is known as krokodil, or "crocodile". It is desomorphine, a synthetic opiate many times more powerful than heroin that is created from a complex chain of mixing and chemical reactions, which the addicts perform from memory several times a day. While heroin costs from £20 to £60 per dose, desomorphine can be "cooked" from codeine-based headache pills that cost £2 per pack, and other household ingredients available cheaply from the markets.

It is a drug for the poor, and its effects are horrific. It was given its reptilian name because its poisonous ingredients quickly turn the skin scaly. Worse follows. Oleg and Sasha have not been using for long, but Oleg has rotting sores on the back of his neck.

"If you miss the vein, that's an abscess straight away," says Sasha. Essentially, they are injecting poison directly into their flesh. One of their friends, in a neighbouring apartment block, is further down the line.

"She won't go to hospital, she just keeps injecting. Her flesh is falling off and she can hardly move anymore," says Sasha. Photographs of late-stage krokodil addicts are disturbing in the extreme. Flesh goes grey and peels away to leave bones exposed. People literally rot to death.

Russian heroin addicts first discovered how to make krokodil around four years ago, and there has been a steady rise in consumption, with a sudden peak in recent months. "Over the past five years, sales of codeine-based tablets have grown by dozens of times," says Viktor Ivanov, the head of Russia's Drug Control Agency. "It's pretty obvious that it's not because everyone has suddenly developed headaches."

Heroin addiction kills 30,000 people per year in Russia – a third of global deaths from the drug – but now there is the added problem of krokodil. Mr Ivanov recalled a recent visit to a drug-treatment centre in Western Siberia. "They told me that two years ago almost all their drug users used heroin," said the drugs tsar. "Now, more than half of them are on desomorphine."

He estimates that overall, around 5 per cent of Russian drug users are on krokodil and other home-made drugs, which works out at about 100,000 people. It's a huge, hidden epidemic – worse in the really isolated parts of Russia where supplies of heroin are patchy – but palpable even in cities such as Tver.

It has a population of half a million, and is a couple of hours by train from Moscow, en route to St Petersburg. Its city centre, sat on the River Volga, is lined with pretty, Tsarist-era buildings, but the suburbs are miserable. People sit on cracked wooden benches in a weed-infested "park", gulping cans of Jaguar, an alcoholic energy drink. In the background, there are rows of crumbling apartment blocks. The shops and restaurants of Moscow are a world away; for a treat, people take the bus to the McDonald's by the train station.

In the city's main drug treatment centre, Artyom Yegorov talks of the devastation that krokodil is causing. "Desomorphine causes the strongest levels of addiction, and is the hardest to cure," says the young doctor, sitting in a treatment room in the scruffy clinic, below a picture of Hugh Laurie as Dr House.

"With heroin withdrawal, the main symptoms last for five to 10 days. After that there is still a big danger of relapse but the physical pain will be gone. With krokodil, the pain can last up to a month, and it's unbearable. They have to be injected with extremely strong tranquilisers just to keep them from passing out from the pain."

Dr Yegorov says krokodil users are instantly identifiable because of their smell. "It's that smell of iodine that infuses all their clothes," he says. "There's no way to wash it out, all you can do is burn the clothes. Any flat that has been used as a krokodil cooking house is best forgotten about as a place to live. You'll never get that smell out of the flat."

Addicts in Tver say they never have any problems buying the key ingredient for krokodil – codeine pills, which are sold without prescription. "Once I was trying to buy four packs, and the woman told me they could only sell two to any one person," recalls one, with a laugh. "So I bought two packs, then came back five minutes later and bought another two. Other than that, they never refuse to sell it to us, even though they know what we're going to do with it." The solution, to many, is obvious: ban the sale of codeine tablets, or at least make them prescription-only. But despite the authorities being aware of the problem for well over a year, nothing has been done.

President Dmitry Medvedev has called for websites which explain how to make krokodil to be closed down, but he has not ordered the banning of the pills. Last month, a spokesman for the ministry of health said that there were plans to make codeine-based tablets available only on prescription, but that it was impossible to introduce the measure quickly. Opponents claim lobbying by pharmaceutical companies has caused the inaction.

"A year ago we said that we need to introduce prescriptions," says Mr Ivanov. "These tablets don't cost much but the profit margins are high. Some pharmacies make up to 25 per cent of their profits from the sale of these tablets. It's not in the interests of pharmaceutical companies or pharmacies themselves to stop this, so the government needs to use its power to regulate their sale."

In addition to krokodil, there are reports of drug users injecting other artificial mixes, and the latest street drug is tropicamide. Used as eye drops by ophthalmologists to dilate the pupils during eye examinations, Dr Yegorov says patients have no trouble getting hold of capsules of it for about £2 per vial. Injected, the drug has severe psychiatric effects and brings on suicidal feelings.

"Addicts are being sold drugs by normal Russian women working in pharmacies, who know exactly what they'll be used for," said Yevgeny Roizman, an anti-drugs activist who was one of the first to talk publicly about the krokodil issue earlier this year. "Selling them to boys the same age as their own sons. Russians are killing Russians."

Zhenya, quietly spoken and wearing dark glasses, agrees to tell his story while I sit in the back of his car in a lay-by on the outskirts of Tver. He managed to kick the habit, after spending weeks at a detox clinic ,experiencing horrendous withdrawal symptoms that included seizures, a 40-degree temperature and vomiting. He lost 14 teeth after his gums rotted away, and contracted hepatitis C.

But his fate is essentially a miraculous escape – after all, he's still alive. Zhenya is from a small town outside Tver, and was a heroin addict for a decade before he moved onto krokodil a year ago. Of the ten friends he started injecting heroin with a decade ago, seven are dead.

Unlike heroin, where the hit can last for several hours, a krokodil high only lasts between 90 minutes and two hours, says Zhenya. Given that the "cooking" process takes at least half an hour, being a krokodil addict is basically a full-time job.

"I remember one day, we cooked for three days straight," says one of Zhenya's friends. "You don't sleep much when you're on krokodil, as you need to wake up every couple of hours for another hit. At the time we were cooking it at our place, and loads of people came round and pitched in. For three days we just kept on making it. By the end, we all staggered out yellow, exhausted and stinking of iodine."

In Tver, most krokodil users inject the drug only when they run out of money for heroin. As soon as they earn or steal enough, they go back to heroin. In other more isolated regions of Russia, where heroin is more expensive and people are poorer, the problem is worse. People become full-time krokodil addicts, giving them a life expectancy of less than a year.

Zhenya says every single addict he knows in his town has moved from heroin to krokodil, because it's cheaper and easier to get hold of. "You can feel how disgusting it is when you're doing it," he recalls. "You're dreaming of heroin, of something that feels clean and not like poison. But you can't afford it, so you keep doing the krokodil. Until you die."
« Last Edit: January 23, 2012, 10:33:55 PM by therepublicanpartier »