AlsoTapered
Bluelighter
- Joined
- Apr 1, 2023
- Messages
- 3,076
As I pointed out elsewhere, the drug we call tramadol is actually two enantiomers. Third party researchers have patented simple ways to resolve the two enantiomers (the researchers wrongly predicted the makers of tramadol would eventually dump the dangerous enantiomer). There are dozens of papers and patents detailing this resolution using tartaric acid and derivatives thereof and it's safe to say that such resolution could happily be carried out in 55 gallon drums using DCM/methanol as the solvent.
If one resolves and then O-demethylates, one ends up with (S) O-DMT which is a classic opioid as potent as morphine. It's well worth reading:
US Patent 5733936A '6-dimethylaminomethyl-1-phenyl-cyclohexane compounds as pharmaceutical active ingredients'
In the table on column 19 of the patent, Example 9 is (+)-(1S,2R)-3-(2-dimethylaminomethyl-cyclohexyl)-phenol hydrochloride.
The analgesic activity (ED50) of tramadol is given as 13.60 mg/kg, the value for example 9 ((S)-ODMT)) is 1.13 mg/kg i.e. 12x more potent.
I'm well aware that Example 2 has an ED50 of just 0.64mg/kg but unless someone can show me a low-tech way of replacing a tertiary hydroxyl moiety with a tertiary fluorine, Example 9 clearly seems the the more facile option.
So I would be MOST surprised if someone hasn't noted how cheap tramadol is, how simple the chemistry involved to resolve it and to perform a simple O-demethylation.
Obviously since you have no need of the (R) enantiomer, 1Kg of tramadol would only yield about 450g of (S)-ODMT but at even $81 a Kg, I do not see this as an issue. IF the price rose dramatically, I'm certain someone with a death wish would step up and fluorinate the product, but I, for one, cannot envisage just how high the price would have to get and how desperate the cooks would have to be to use DAST at scale.
It IS noted that trans tramadol (not found in the medicine) can be racemized and it would be interesting to discover if the waste (R) tramadol can be racemized. After all, in both Europe and Mexico methamphetamine cooks have been observed resolving the two enantiomers of the drug and racemizing the unwanted isomer. If possible, that seems far more likely than crazy people playing with DAST.
Last word - over 140 tonnes of tramadol are produced each year hence the low price of the drug. But it doesn't require the poppy.
Obviously the above would be totally illegal in the UK but I'm unsure of the laws elsewhere BUT I am just laying out the fact that (S)-ODMT doesn't require the poppy,
If one resolves and then O-demethylates, one ends up with (S) O-DMT which is a classic opioid as potent as morphine. It's well worth reading:
US Patent 5733936A '6-dimethylaminomethyl-1-phenyl-cyclohexane compounds as pharmaceutical active ingredients'
In the table on column 19 of the patent, Example 9 is (+)-(1S,2R)-3-(2-dimethylaminomethyl-cyclohexyl)-phenol hydrochloride.
The analgesic activity (ED50) of tramadol is given as 13.60 mg/kg, the value for example 9 ((S)-ODMT)) is 1.13 mg/kg i.e. 12x more potent.
I'm well aware that Example 2 has an ED50 of just 0.64mg/kg but unless someone can show me a low-tech way of replacing a tertiary hydroxyl moiety with a tertiary fluorine, Example 9 clearly seems the the more facile option.
So I would be MOST surprised if someone hasn't noted how cheap tramadol is, how simple the chemistry involved to resolve it and to perform a simple O-demethylation.
Obviously since you have no need of the (R) enantiomer, 1Kg of tramadol would only yield about 450g of (S)-ODMT but at even $81 a Kg, I do not see this as an issue. IF the price rose dramatically, I'm certain someone with a death wish would step up and fluorinate the product, but I, for one, cannot envisage just how high the price would have to get and how desperate the cooks would have to be to use DAST at scale.
It IS noted that trans tramadol (not found in the medicine) can be racemized and it would be interesting to discover if the waste (R) tramadol can be racemized. After all, in both Europe and Mexico methamphetamine cooks have been observed resolving the two enantiomers of the drug and racemizing the unwanted isomer. If possible, that seems far more likely than crazy people playing with DAST.
Last word - over 140 tonnes of tramadol are produced each year hence the low price of the drug. But it doesn't require the poppy.
Obviously the above would be totally illegal in the UK but I'm unsure of the laws elsewhere BUT I am just laying out the fact that (S)-ODMT doesn't require the poppy,