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#7 ALEPH-7
2,5-DIMETHOXY-4-(n)-PROPYLTHIOAMPHETAMINE
SYNTHESIS: A
solution of 2.6 g
2,5-dimethoxy-4-((n)-propylthio)benzaldehyde (see under
2C-T-7 for its
synthesis) in 20 mL
nitroethane and 0.5 g
anhydrous ammonium acetate
was heated on the steam bath overnight. The excess
solvent/reagent
was removed under vacuum leaving an orange oil as a residue that
cry-stallized spontaneously. This crude product was re
crystallized
from 20 mL boiling MeOH to give, after cooling, filtering, and air
drying, 2.4 g of
1-(2,5-dimethoxy-4-(n)-propylthiophenyl)-2-nitropropene as orange
crystals. Its mp was 83-84 °C with prior sintering at 81 °C.
A suspension of 1.5 g LAH in 150 mL of warm
anhydrous THF was stirred
under an inert
atmosphere and brought up to a gentle reflux. A
solution of 2.3 g
1-(2,5-dimethoxy-4-(n)-propylthiophenyl)-2-nitropropene in 25 mL
anhydrous THF was added dropwise at a rate that maintained the reflux.
Heating and stirring were continued for 2 days, and then the reaction
mixture was allowed to stir at room tem
perature for an additional 2
days. There was added 1.5 mL H2O (
dissolved in 10 mL THF), followed
by 1.5 mL 15%
NaOH, and finally another 4.5 mL H2O. Stirring was
continued until all the curdy solids had turned white. The reaction
mixture was filtered, and the filter cake washed with slightly wet
THF. The filtrate and the washings were combined, and the
solvent
removed under vacuum. The residue was about 2 mL of an amber colored
oil that was
dissolved in 200 mL
CH2Cl2. This
solution was washed
with first dilute
NaOH, and then with saturated brine. Removal of the
solvent gave a pale amber oil that was
dissolved in 10 mL IPA,
neutralized with about 14 drops of concentrated HCl, and diluted with
200 mL
anhydrous Et2O. The clear
solution was decanted from a little
gritty material, and then set aside to allow the formation of
2,5-dimethoxy-4-(n)-propylthioamphetamine hydrochloride (ALEPH-7) as
fine white
crystals. After filtration and air drying, there was
obtained 1.8 g of an off-white powder.
DOSAGE: 4 - 7 mg.
DURATION: 15 - 30 h.
QUALITATIVE COMMENTS: (with 4 mg) At the second hour I had a
paraesthetic twinge or two (all pins and needles), and then felt quite
relaxed, quite willing to let this play itself out. In the evening my
ears still feel 'popped' and there is a little bit of physical
awareness. There is not much fun with this. The night following, I
was unable to sleep and only dozed slightly, but I seemed to be OK the
next day.
(with 6 mg) The alert was felt within a half hour, and then nothing
more. Then, over the next two hours, there was the evolution of an
extremely neutral state. I danced wildly to a record of Keith
Jarrett, but somehow didn't care for his style. I fell apart
emotionally, with tears and a feeling of total loss of everything.
Everything was visible to me only in some strange wide-angle lens
viewing. I went for a walk, a waste of time. I tried classical
music, but only jazz was acceptable. It was a couple of days before I
lost the
residual strangeness feeling. Never again.
(with 7 mg) I did this alone, and in retrospect I wish I had not.
Somewhere between the hours 2 and 3, I got to a full +++, and I was
concerned that I saw the effects still developing. Where would it go
now? There was no reality loss as with LSD, no shakes or shimmers,
but an intense and profound +++ of something characterized only by the
absence of extremes. And I am frightened because this is still
deepening. A couple of calls to friends were not successful, but I
found an ally in the Palo Alto area, and I told him I was coming to
visit. My greater than one hour drive there was okay only because I
had programmed every move ahead of time. In retrospect, to drive was
completely stupid, and I certainly will never do it again, under any
circumstances. But, there I was. I knew which lane I would be on, on
the S.F. Bay Bridge, at every moment of my travels. The middle lane
through the tunnel. The second from the left when descending into San
Francisco. The white lane-marker stripes were zipping up past my
lateral field of vision as I drove, those that were to my right zipped
past my right eye, those to the left past my left eye. Like disturbed
fruit flies leaving an over-ripe peach. But, as everything had been
preprogrammed, there were no surprises. I made it successfully, and
my baby-sitting friend probed, with a blend of curiosity, love, and
envy, my uncaring state. And in the course of the next couple of
hours, this state evolved into a friendly, familiar place. I was
still fully +++, but now for the first time I was at peace with it. A
fruit salad tasted heavenly. By midnight I was able to doze lightly,
and the next day I was sure that there were some
residual effects.
The second evening's sleep repaired everything. The neutralness was
something new to me. I don't like not caring. Was this the "Beth"
state of the strange twenty minutes seen by SL in the ALEPH-4
experience?
(with 7 mg) Strange, pleasant, unexciting, long-lasting. The induced
state was characterized by: clear unintoxicated central field of
vision, concentration but with the
periphery sensed as being filled
with a kind of strangeness, and also something sensed inside, at the
back of the head. A feeling of something waiting to erupt, which
never does. I had a faint touch of amusement, yet no part of the
experience had the depth or richness of other compounds. No tremors.
Slight visuals, but only when looked for. Hunger not present, but
food tasted fine when eaten. Mildly pleasant but one would not take
it again unless bored stiff.
EXTENSIONS AND COMMENTARY: This drug was the first definition of the
term, Beth state.
There is something of the Fournier Transform in any and all drug
experiments. A
psychedelic drug experience is a complex combination
of many signals going all at the same time. Something like the sound
of an oboe playing the notes of the A-major scale. There are events
that occur in sequence, such as the initial A, followed by B, followed
by C-sharp and on and on. That is the chronology of the experience,
and it can be written down as a series of perceived
phenomena. The
notes of the scale. Black quarter notes, with flags at the tops of
their staffs, going up the page of music.
But within each of these single events, during the sounding of the
note "A," for example, there is a complex combination of harmonics
being produced at the same time, including all components from the
fundamental
oscillation on up through all harmonics into the
inaudible. This mixture defines the played instrument as being an
oboe. Each component may be shared by many instruments, but the
particular combination is the unique signature of the oboe.
This
analogy applies precisely to the study of
psychedelic drugs and
their actions. Each drug has a chronology of effect, like the notes
of the A-major scale. But there are many components of a drug's
action, like the harmonics from the fundamental to the inaudible
which, taken in concert, defines the drug. With musical instruments,
these components can be shown as sine waves on an
oscilloscope. One
component, 22%, was a sine wave at a frequency of 1205 cycles, and a
phase angle of +55!. But in
psychopharmacology? There is no
psychic
oscillo-scope. There are no easily defined and measured harmonics or
phase angles. Certainly, any eventual definition of a drug will
require some such
dissection into components each of which makes some
contri
bution to the complex whole. The mental process may some day be
defined by a particular combination of these components. And one of
them is this Beth state. It is a state of uncaring, of anhe-donia,
and of emotionlessness.
Many drugs have a touch of this Beth state, ALEPH-7 more than most.
If a sufficient
alphabet of effects (I am using the Alephs, Beths,
Gimels, and Daleths of the
Hebrew as token starters only) were to be
accumulated and defined, the actions of new materials might someday be
more exactly documented. Could
depression,
euphoria, and
disinhibition for example, all be eventually seen as being made up of
their component parts, each contributing in some measured way to the
sum, to the human experience? The
psychologists of the world would be
ecstatic. And drugs such as ALEPH-7 might be useful in helping to
define one of these parts.
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