SYNTHESIS: A solution of 8.4 g 2,5-dimethoxyamphetamine base in 40 mL
acetic acid was added dropwise over the course of 0.5 h to 43 mL of
50% nitric acid which was well stirred and cooled with an external ice
bath. The resulting solution was quenched with ice water, made basic
with aqueous NaOH, and extracted with a benzene-ether mixture. The
residue that remained after the removal of the solvent was dissolved
in dilute HCl which, upon evaporation of the H2O, yielded a nearly
colorless residue. Recrystallization from an ethanol/ether mixture
gave, after drying, 10.5 g of 2,5-dimethoxy-4-nitroamphetamine
hydrochloride (DON) with a mp of 206-207 °C. The acetamide derivative
melted at 166-168 °C. The formamide derivative was easily hydrolyzed
with 3N HCl. And the R-isomer of DON hydrochloride had a mp of
231-232 °C.
DOSAGE: 3.0 - 4.5 mg.
DURATION: 8 - 15 h.
QUALITATIVE COMMENTS: (with 3.0 mg) There was an amphetamine-like
stimulation that was apparent an hour into it, and considerable
anxiety. I had stomach cramps, but there were indications that there
might be something hallucinogenic at a higher dose.
(with 4.5 mg) An enhancement of color perception, and some auditory
distortion, that was still noticeable some eight hours into the
experience. The visual changes were intense. I felt I was running a
slight fever, and was restless, but there was almost no physical
malaise. I was still somewhat wound up even at the 14th hour.
EXTENSIONS AND COMMENTARY: These qualitative comments are not true
quotations, but have been reconstructed from the published summaries
of the human trials reported by several South American researchers. I
have personally never tasted DON and have only these fragments from
which to create a portrait of activity. A brief quotation, from a
note published by these researchers in a bulletin that is restricted
to forensic scientists serving law enforcement agencies, is certainly
subject to a number of interpretations. It reads as follows: "This
action [a strong stimulant action reminiscent of amphetamine] seems to
reduce the incidence of insightful, and therefore potentially
unpleasant experiences, and thus [DON seems likely] to appear on the
market as an illicit recreational drug." I must admit that I have
tried, and I am still not able, to interpret this quotation.