Александр Шульгин II
Specific: A novel phenethylxanthine-type stimulant was synthesised in extremis, characterised in vivo and tested in corpore meo. Simple, locally-sourced organic precursors were employed, and the synthesis was conducted in an artisanal camper- van kitchen. The purity of the product was established by molecular gustometry as being of the highest order. Finally, chemopsychological studies indicated that the compound has pronounced effects on mood, concentration, productivity and will-to-live.
Introduction
Due to a complex series of events spanning approximately three years, four months and 14 days, our research team (n = 1) was tasked with writing an 80,000 word document in six weeks. Such a task poses a significant challenge, physically, mentally and pharmacologically. A cursory literature review indicated a profound absence of psychoactive substances capable of facilitating such a feat.1 Substances available over-the-counter have insufficient potency, while under-the-counter alternatives are beset with side-affects and purity issues.
This lack of viable alternatives kickstarted this research, which culminated with with the synthesis of a novel compound, Caphetamine. This molecule was then tested for activity on a small sample population (n = 1) and was shown to have significant attention- and productivity-boosting properties.
Project Timeline
Given the short available timeframe, we allocated a week for drug design and retrosynthetic analysis, and a further week for the synthesis itself. This left three weeks of intense writing, and the last week as leeway for any setbacks (Figure 1).
Selection of Target Compound
Seven days was insufficient time for a conventional high- throughput screening approach. Instead, we opted for a linear combination of existing stimulants. Legality, price, availability and eBay delivery time were factored into the selection of starting materials, which in turn determined the nature of the target (Figure 2).
We settled on the structure shown in Figure 2, a 1:3 composite of caffeine and amphetamine (Adderall). We anticipated that our drug would combine the heightened cognition, focus and drive of amphetamine with the minimal addictiveness of caffeine, while also being three times as potent. We should specify, however, that we have no formal training in biomedical research or pharmacology.
Retrosynthetic Analysis
Sleep deprived as we were, the synthesis of caphetamine seemed at first like a Gordian Knot.2 Inspired by the work of another Alexander, we decided to split the whole thing down the middle.3 This resolved caphetamine into a pair of more approachable precursors: dialkylurea 2 and imidazole 3. We anticipated that urea 2 could be prepared from Adderall and phosgene, while a condensation reaction could deliver 3.
Stereochemistry
Seriously? You think we had time for that shit?
Forwards Synthesis
The first challenge we encountered was sourcing amphetamine. As this study was conducted during finals week, every pharmacy within 100 km of our institute was sold out of Adderall. Ligma- Balldrich’s price was prohibitively high, (over $1600 per gram),4,5 so we had to resort to other means. We obtained 3 g of the N-methyl derivative (4) from a local organic chemistry startup (Skinny Pete’s Fine Chemicals). This material was then demethylated with a heterogeneous yttrium catalyst.6 The reaction was supposed to be monitored by TLC, but we fell asleep, and the product was collected from the ceiling of the fume hood the next morning. Characterisation was done via a taste test, and the product was “tight tight tight”.7
The amphetamine thus obtained was reacted with phosgene, which was generated in situ from the combustion of carbon tetrachloride (Scheme 2).8 This reaction delivered urea 2 in a yield higher than your uncle at thanksgiving dinner. To prevent over-reaction (or other forms of chemical hysteria) in subsequent steps, 2 was cyclised with bromomethyl fmoc to give compound 10.
To prepare the imidazole, we used a Schplatt-Inglfinger-Künz condensation of amphetamine, hydroxyacetone and formamide, a reaction that looks exactly like it sounds. A subsequent oxidation with potassium chromanganate delivered intermediate 3 alongside a slurry of vile-smelling tar.
With intermediates 10 and 3 in hand, we began the process of joining them in holy heterocyclimony. The first step was a hydrogenolysis of half 10’s FmocMe group, catalysed by palladium-on-lemon,9 followed by a modified peptide coupling with 3. We got the FmocMe off with piperidine, and then performed a novel Margit-Godrick-Radhan iron-catalysed dehydrogenative coupling to obtain the final product.10 Purification was performed by recrystallising the crude material from hot silicon oil, which yielded an off-white solid.
Biological activity test methodology
The biological activity of the synthesised compound was extensively tested across a three-week period. The participant was given a small initial does of Caphetamine to test its safety. ECG and blood pressure readings were taken to monitor the patient’s health. After the compound was administered, the patient’s cognitive performance was measured using several methods. To test intellectual capacity, the standard New York Times daily games and the Human Benchmark assay screen were employed. Fine motor skills were assessed by Lego Death Star Building (LDSB).
Results and Discussion The results of this study were incredibly satisfactory. Firstly, the volunteer reacted well to the drug with effects appearing only a few seconds after ingestion. The patient’s ECG trace was unusual (Figure 3), and their blood pressure was higher than a Tour de France cyclist’s, but this did not appear to concern them.
The NYT test returned results that were also better than expected. The sudoku was completed with a time of 1:23 minutes and the wordle only took three attempts. The spelling bee, on the other, hand was not completed in a satisfactory manner. Exceptional (99th percentile) results were obtained in the reaction time test, while the number memorisation section was cut short due to lack of time. The aim trainer test was also performed for the sake of scientific integrity, and it was found that the patient’s focus and speed put them in the Immortal II percentile of the Valorant scale, despite being hard-stuck copper III. Finally, the LDSB test yielded satisfying results. This test typically spans over several days, but the patient completed it in a matter of hours. They stayed focused on the task unphased by any outside stimuli or distractions, including two fire alarms and an earthquake.
The duration of the novel compound’s effects was approximately one afternoon. Movement twitchiness reduced approximately four hours after ingestion, and blinking became possible again shortly after. The vitals of the patient returned to standard levels about 8 hours after the start of the experiment.
It must be noted that the author felt a strong urge to test the compound again, just to be sure the results were accurate. However, as they had left their access-card inside the lab after hours, they had no choice but to wait until the next morning (after clawing at the windows and squawking for a while). When circumstances permitted, the series of experiments was repeated several times, and similar results were obtained.
The effects on attention span and productivity of the synthesised compound were astounding. This research was performed with the goal of synthesising a stimulant that would allow for the writing of circa 80 000 words in the span of four weeks. This required intense focus for extended periods of time with minimal downtime (sleeping, eating, showering, blinking). When work on this project was conducted under the influence of Caphetamine, a significantly higher level of productivity was obtained than with other stimulants (Figure 4).
Effects on Attention Span and Productivity
It’s effects on work performed per unit time was found to be almost nine times more potent than caffeine and 2.5 time more potent than an angry email from a supervisor. Words typed per- day almost doubled and thoughts-per-second were increased by a factor of a lot. The major contributor to this was the drastic reduction in sleep time (10 hours a week on average) with minimal loss of ability to focus and write in a professional manner.
The author describes the sensation as being like dry-scooping pre-workout whilst being mildly electrocuted.
Conclusion
The thesis was written in 3 weeks and 2 days. Nuff said.
Experimental details/electronic unsupported information are available from: https://www.TotallyLegitData.com/NotABitcoinMiningVirus
Acknowledgements
А. Ш. acknowledges the voices in his head for helpful discussions, as well as the dealer from around the corner.
Notes and references
1 https://tinyurl.com/3yun2ne6
- https://en.wikipedia.org/wiki/Gordian_Knot
- “A Retrosynthesis of Gordiane Alkaloids” Alexander O. Macedon, Phillip O. Macedon, 333 BC, Phrygian J. Chem. III, 356–323.
- https://www.sigmaaldrich.com/AU/en/product/usp/1180004
- “Making the Most Out of Your Research Funding: Raney “Nickel” M. Rotch, S. Butz, A. Bath, T. T. Culis, 2024, J. Immat. Sci. 4, 1.
- “A Novel N-Demethylation Catalyst: Y2O5InK” P. Pugh, M. Pugh, B. McGrew, 2023, J. Camp. Chem. 24, 7–8.
- “On the purity of phenethylamines” T. Salamanca, 2008 Bromine and Barium Chem., S1E7.
- Note: CCl4 was extracted from a 1960’s fire extinguisher.
- “Applications of Lemons in Synthetic Chemistry” Jiugui, Y. Wang, 2024, J. Immat. Sci., 4, 37–39. https://jabde.com/wp-content/uploads/2024/07/Lemons.pdf
- “Novel and Facile Haemoglobin-Catalysed Cross-Coupling” S. Radahn, F. O. Margit, G. Godrick, 1050, J. Lim. Swamp. Chem., 38, 450–475.