Dichloromescaline

by The Inner Frontiersman and Toad

Toad's Voice:

Dear Friends, I thought I'd pass along a most interesting report that was published in the latest Entheogen Review. The report is certainly lacking some key information, but from the sound of it the mysterious author could really be on to something. I will follow up this report with a transcript of the proper Lloydia paper that was incorrectly referanced in the E.R. report. Once the groundwork has been layed out, I'd like to open up a discussion about the possible conversion techniques and chemistry questions...

Here is the original report written by the Inner Frontiersman from the Vernal Equinox 1997 Entheogen Review in most of it's entirety:

"First Known Human Voyage on DCM -- 2,6-dichloromescaline"

Dekorn writes: On Page 7 of the Spring 96 ER is a piece by the following author, speculating on how to make 2,6-dichloromescaline. This previously uninvestigated compound, a presumed "super entheogen" was first mentioned in Lloydia, Vol. 40, No.6 in an article entitled "Cactus alkaloids XXXVI. Mescaline and related compounds from Trichocereus peruvianus" (**Dekorn had cited the wrong title here which I have corrected**) The article's authors speculated that on the logic of molecular chemistry alone, 2,6-dichloromescaline should be "well within the range where psychoactivity would be expected." Not to be daunted, our intrepid psychonaut took the considerable trouble to make some and here are his results...

Inner Frontiersman writes: After spending a small fortune to isolate the pure mescaline, then convert it to DCM, I gave myself two weeks to mentally prepare. All the information was theoretical -- it could be a dud, it could be a psychotic agent, or it could be a super entheogen. I decided to start the test at 4:30 AM, three hours before sunrise on April 26, 1996.

4:30 AM 10mg DCM
5:00 AM Nothing
5:30 AM Nothing
5:45 AM Nothing
6:00 AM + 1
6:30 AM + 2.5
6.45 AM + 3.5

At this point the intensity was rocketing past the equivalence of 2 full window panes = 300 mcg. LSD. Things dissolved and dissasembled. I could see my consciousness separate into a dozen or so points in space. My eyes, and every other element of consciousness were all "thinking" on their own. I had the ultimate terror that I was dissasembling into nothingness, but suddenly, this struck my emotional essance as highly comical. This laughter spread through all of my other essences like a pencil links each dot in a connect the dot puzzle.

This was a grand awakening voyage. At one point I experianced what could only be called a "mental sex change". I percieved myself as both physically and mentally female. After a brief wave of terror, I realized that, without going into great explanation, there is power in being female.

A vision of what I could only reason was that of the Creator's followed. Both extreme terror and total peace and happiness filled me. I saw a pastel rainbow hue of colors. In the middle of these colors a beam of golden light projected outwards towards me. When it struck, I felt only the peace and joy of the beam as well as heard a voice that said many things. The only phrase I remember was "Do not be tricked by the evil ones that inhabit other realms, resist them, and they will flee in terror, they only have the power you give them!"

There was an image of a small frog like creature belching out the usual phrases to intimidate psychonauts. I laughed uncontrollably at this pathetic little evil "thing" until I hurt. It then vanished. The rest of the voyage was filled with nice visuals, great euphoria.

The total elapsed time breaks down as follows: From plus-1 to plus-1, about 22 hours. The plus-2 state lasted about 13 hours, and the plus-3 portion of the trip was about 9.5 hours. The only problems were intermittent power surges through my body, with both feelings of electricity and some trembling. This was on a dosage of only 10mg! I wouldn't take this amount again-- I was lucky. A recomended starting dose would be 3-5mg. Note: all of my DCM notes and formulas were destroyed in an electrical fire about 2 weeks later! I had plans for a psychedelic salve: about 1mg of DCM in DMSO. The fire stopped this, at least for now. Due to the molecular structure of DCM, DMSO should be an excellent vehicle for delivery. Hopefully someone with better scales and equipment will give a good scientific investigation of DCM.

-Inner Frontiersman

Toad's Voice: The Inner Frontiersman then goes on to speculate about various conversion methods without saying exactly how he produced the final DCM product. He also makes an error in his interpretation of the Lloydia paper stating that the DCM was an artifact from trying to purify mescaline HCL using chloroform as a separating solvent. The paper actually stated that 2-chloromescaline was the artifact and they later created DCM in a separate procedure.

Inner's report continued:

2,6-dichloromescaline was an artifact from trying to purify mescaline HCL by using chloroform as the separating solvent. It seems that the chloroform has some free radical Cl ions available and by accident, they bound to the mescaline. They found this residue, about 3% conversion during some chemical tests. The conversion happened over an 8 hour period.

The first route to 2,6-dichloromescaline would be to take nearly pure crystals generated by the easy extraction method and dissolve them in chloroform, about one pint to 300mg. Then add the catalyst to speed up the chloroform's formation of free Cl, potassium permanganate, about 200mg. Allow this to set for one full day, which will give time for the conversion. 97%. (This is not the procedure from the Lloydia paper. If this is the procedure he followed then there would be 40% potassium permanganate in the final product that would need to be removed somehow).

The simpler method would be to dissolve 300mg of mescaline in one liter of chloroform in a sealable glass container and let it sit for a month, allowing the chloroform to release the Cl as part of its natural decay. Once a week you'd open the container to let the voatile hydrocarbons out: being careful not to inhale them. Probably six weeks at 72 degrees would yeild better results. You want to ensure that all the solids stayed in solution by regular stirring or shaking. If you started with a reletively pure product, you could allow the chloroform to evaporate off leaving the DCM as residue.

A note on dosage: I checked the calibration of my old triple-balance scale against two others and discovered and error between 6 and 21 mg with no consistant pattern! Which means that my "10mg" dose could have been anywhere from 6 and 21mg. This stuff gave all the weird electric power surges similar to what I have read in Dr. Shulgin's descriptions of many of the psychedelic amphetamines. At times I felt like I was strapped to the front of a runaway locomotive: this is a very very pushy material! I don't know anyone who has braved high dose STP (DOM), but maybe they have some tips to prevent tragedies. Start with a low dose would be my plea to anyone interested in DCM. This is not high-dose mushroom madness, or peyotehuasca music of the spheres! In other words, although I had a great time, if I had fought in the least bit, it woud probably have put me through a mental and spiritual food processor. The only favor that I ask is that someone you know and trust who can get the Lloydia recipie for DCM and verify that it is a psychedelic trip and not poison.

-Inner Frontiersman


Taken from Lloydia Vol. 40 No.6 "Cactus Alkaloids XXXVI. Mescaline and Related Compounds from Trichocereous peruvianus" (p585)

Preparation of 2-chloromescaline and 2,6-dichloromescaline hydrochlorides. Chlorine gas was generated from potassium permanganate and hydrochloric acid, and a 5% (w/v) solution was prepared in chloroform. A total of 150mg of mescaline hcl was disolved in 100ml of chloroform to which 1ml of the chlorine solution was added. After the mixture was kept at room temperature for 2 hours the solvent was removed under rotary vacuum (only 2,6-dichloromescaline was formed if the mixture was kept for longer periods of time). The residue was treated in the usual manner to crystalize 120mg of hydrochloride (shiny plates, mp 218-22). Recrystalization (absolute ethanol-ethyl ether) purified this material, which was identified as 2,6-dichloromescaline hydrochloride mp 225-227. The mother liquor from the crystalization of the 2,6-dichloromescaline hydrochloride showed three spots upon analytical tlc in solvent (ethyl acetate-methanol-58% ammonium hydroxide (17:2:1)) at 0.36, 0.55, and 0.77

The mixture (90mg) from similar mother liquors was subjected to preparative tlc (three plates, two developments). The band at Rf 0.36 yielded 26mg of recovered mescaline hydrochloride; the band at 0.77 gave 36mg of additional 2,6-dichloromescaline identical to that obtained previously. The band at Rf 0.55 yielded 15mg of 2-chloromescaline hydrochloride.


Toad's Voice:

I gladly present the following brief synopsis and data-points to finally bring the 2,6-dichloromescaline saga to completion.

The 2,6-dichloro and the mono-chloro mescaline derivatives were not active in the 3-10mg range as described in the Entheogen Review article by the Inner Frontiersman. The article was a hoax, and most likely based upon the predicted activity of these compounds by structure activity relationships.

Both 2,6-dichloro and the mono-chloro compounds were active in humans in dosages greater than 75mg. One experimenter found 150mg of the mono-chloro compound to be psychoactive. The experimenter involved was not overly impressed with the effects elicited, and said that he was not interested in exploring things any further.

The 2,6-dibromo and mono-bromo compounds seemed to be more interesting. I had the opportunity to taste the mono-bromo, and found 130mg to be a fully active amount for me. It elicited an enjoyable psychoactive state that reminded me of 2cb without the stimulating bzzz. While my trials of this material were encouraging, it definitely pales in comparison to the ancient mescaline diamond and therefore leaves me asking the question "why bother".

The iodo derivative was also prepared and tasted, and the effects from the first effective trial seem to encourage further exploration.

Toad