I’ve spent the past 15 years consumed by the fiery passion of chemistry, which has defined my career as well as my clandestine destinies. Chemical creativity is different from that of the artistic varieties. There are very few truly brilliant chemists, i.e. the Linus Paulings of the world, who lay the foundations for and invent concepts that create new branches of the field. The best that most chemists can aspire to be is a highly resourceful, well-read, masterful technician. The ones w/ dozens of patents and their own firm, the top 1%, are brilliant masters of the pooled intellectual resources of the greater chemical community, being able to borrow related concepts and methodology from analogous rxns and apply them in novel ways to pre-existing commercially important compounds, or using known tools to develop novel molecules. We patent and invent “novel” methods/molecules, mostly, by borrowing related concepts and methodology from analogous rxns and applying these already established tools to a new molecule. I consider myself to be a highly right-brained individual. I’m more suited for creating art, music, and literature than a career in chemistry. Nonetheless, I find it richly rewarding and couldn’t imagine doing anything else. To me, the whole left-brained analytical process of science was a novelty and an adventure. It still is. At times however, as an artsy-creative type in a very serious analytical field, I feel like I’m a virtual machine running on an OS based on different architecture. The result may look the same, but the process is synthetic. What I cherish the most about my professional life are the more creative outlets and social interactions that come along with being part of a research group, such as presenting and networking at conferences, conveying our ideas in publications, persuading funding bodies to hop on board our train (it makes me feel like a gangster manipulating these pompous committees, board members and private/govt organizations to hand us their money...almost as good as it would feel if they signed a check made out to the Duchess herself), and, of course, I’m passionate as hell about teaching (and, surprisingly, it’s not always motivated by my underlying naughty desires to seduce members of the lacrosse team). But when I take off the lab coat and enter the privacy of my domicile, I feel that I can don my pointy black hat, perhaps a politically incorrect version of “Horny Heroin-Heroine Hermione goes to Hogwarts.” All of this wonderful knowledge, resources and tools at my disposal that can be retooled for a more subversive purpose (“subversive” only b/c society labels it so): for the benefit of members of the clandestine community, members of society, whom, like myself, have a shared secret passion. While the pursuit of better hedonism through chemistry, aka: opio-phoria, is not the same as witchcraft, historically speaking, there are plenty of analogies. They’ve both experienced prohibition, persecution and, thus, share the appeal of forbidden fruit. If you want the Duchess to explore something, simply tell her that she shouldn’t do it. [Footnote #1 in Bibliography]
Curiosity may kill cats, but that’s b/c, unlike me, they only have nine, instead of 40+ lives. They plan their epic explorations of the feline world like pussies. I plan my exploration of the opio-verse like a girl scout: preparing for feral felines disasters, feline distemper, and fentalogue hiccups. When engaged in a clandestine field where self-experimentation is the norm and the development of dependencies and tolerances are pretty much guaranteed, it helps to bring along a chaperone; in my case, a “naloxone chaperone” aka: nalaperone. This traditionally takes the form of a side-kick, partner in crime, partner-of-mine, or, if you believe in naloxone-toting angels, then (perhaps) partners-divine.
Maybe I shouldn’t assume that all of you have seen that cute PSA promoting “responsible analoging,” the one w/ that cute catchphrase:
Would you play a saxophone with a reed made from a scone?
Would you loan a suboxone under the tongue of a sista who’s on methadone?
Would you ride bikes with Eliot w/o helping E.T. Phone Home?
“Auntie’s syringes ain’t daggers,” you remind your 4 y.o. Nephew, “Just leave that shit alone,”
All Niece-nephew dagger fights are accompanied by an auntie w/ nappies and some naloxone,
Yo’ hair ain’t turf; yo’ head ain’t no astro-dome, it’s more than a mere hollow sphere encased in shiny bone,
So when you’re playing the needle-prick-a-phone w/ a novel analogue of oxymorphone,
Or attending poke-a-dilly-circus accompanied by 14-cinnamoyloxycodeinone,
Or wanna safely stone on your latest bezitramide derived ketone,
Don’t go playing Morpho-polo w/o an appointed nalaperone.
To safely navigate intravenous hide-n-seek in the realm of the opio-unknown,
Don’t be no fool, nigga, please don’t analogue alone.
[Footnote #2]
Prior discussions involving naloxone to oxymorphone adapted to the clandestine realm (from what I’ve read) have been restricted to purely theoretical discussions on forums such as The Vespiary, Bluelight, etc. involving some good propositions for N-deallylation, but no experimental procedure or details have been provided. My goal w/ the Narcin’ Out Naloxone Project was to take the lessons that I’ve learned over my years of experimentation with the naloxone conversion, simply them into procedures accessible to the hobbyist and clandestine community, and disseminate them with the same fervor and gusto with which I sip sem…[and they used to say I had a problem with self-control…]. It is a democratization of chemistry and of pharmacology. Adding to the euphoric pharmacopeia, the euphoricopeia, the joys of my favored N-phenethyl darling: phenomorphone. And the whole “Essential Euphoricopeia of the égalitarisme chimique'' part? This is just silly wordplay, an attempt to mix my fictional terminology with important sounding French words so that my fictional ones appear more legitimate.
This monograph summarizes many years of experimental refinement and adaptation of these procedures for the hobbyist. I have prioritized practicality and accessibility over yield and purposefully avoided more advanced procedures, such as preparative-flash chromatography, which, if you have access to, is usually a preferable means of product isolation-purification, but by no means required. You need not have a corporate account w/ a domestic chemical supplier for these reagents. Chemsavers is the individual hobbyists best resource for accessing the entire Thermo-Fisher/Acros, Sigma-Aldrich, TCI, Alfa Aesar (and more) catalogs. There are also numerous domestic hobbyist suppliers, Amazon/eBay, and legit slanty-eyed retailers. Despite the slanty-habit of ripping-and-running in the RC market (like Omar from HBO’s The Wire), there are a plethora of above-board, legitimate Oriental chemical-R&D supply houses that will gladly take your business for anything and everything (exception: controlled substance): they’d happily sell nerve gas to ISIS & fire-&-brimstone to Sodom & Gomorrah, it’s one of the few places left where, as long as your money is green, your business is welcome. Another good international resource is the OG of the multinational R&D: Germany. ABCR and others [
https://www.chembuyersguide.com/chemical-suppliers/germany.html] are eager beavers for your biz. They will sell just about everything to anyone anywhere. Although they may be somewhat reluctant to export VX or sarin gas precursors to ISIS, their French counterparts do have a history of equipping Israel and other nations with easily convertible nuclear breeder reactors (i.e. Atomic Allah Akbar). If you desire that enriched yellowcake fire, you’ll probably need to hide your underground plutonium factories inside a hollowed-out mountain, b/c the Israelis are quite serious about their Nuclear Whack-a-Mullah Doctrine, and are known to have serious boundary issues...that is, the inability to respect international boundaries or sovereignty ;-)
In my “Homegrown Hoboken Heroin” article (see my other Reddit posts), I briefly discussed the chemistry of thebaine derivatives, which belong to either the 14-hydroxymorphinone class or that of the Diels-Alder adduct Bentley compounds. This investigation into N-substituted 14-hydroxymorphinones derived from noroxymorphone by way of N-deallylation of naloxone is especially chemistry-rich. There are multiple procedures available, some of which are derived from work that Her Right Honourable Highness has done by reverse engineering known N-demethylation rxns. You can call these reverse N-deallylations: Duchess von D-allylation. The N-dealkylation of alkaloids (overwhelmingly) involves N-demethylation, but, for most of these same dealkylation reagents, N-deallylation is a lower energy, more preferable rxn compared to that of N-demethylation. For those desiring more chemical lit. and less of my naughty psychobabble lip, this monograph should satiate your craving.
I promise to make this one especially heavy and creamy with an extra special layer of creme-de-la-chemistry. You have probably grown accustomed to the eccentric nature of my monographs, which are peppered with plenty of sarcasm, absurdist parenthetical distractions, and some outlandish musings. Some of you may find it frustrating to wade through my pseudo-psychotic ramblings in order to get through the good stuff. Because bat shit crazy babe-lip is not for everyone, I will do a better job keeping future monographs “clutter free.” My non-chemical musings will be reserved for the postscript, in a section at the end of the monograph. [for more on what I originally put here in my Reddit version of this post, please see Bibliography Footnote #3]
We won’t be dealing with the typical fodder for structure-activity relationship-based discussions of the 14-hydroxymorphinone class, such as the modification of the ketones or the 14-hydroxyl functional group. Instead, I will be sharing a bit of my clandestine-underground-badass-witty-bitty-bitch alchemical secrets: the (non) magical high-efficiency transmutation of naloxone into the promising intermediate noroxymorphone, from which more than a dozen highly potent N-substituted analogues can be derived. My preferred darling doughnut of this baker’s dozen is N-(2-phenethyl)-noroxymorphone, a highly potent full mu-agonist euphoriant with oral euphoric potency of 10 x methadone (but with far less sedation and increased euphoria) and a parenteral potency on par with fentanyl, but w/ improved opio-phoria and a mild stimulant-like giddiness reminiscent of that first line of oxycodone back in high school.
[For more on the origins of some alternative colorful names considered for Phenomorphone, please reference Footnote #4]
Unlike the rapid tolerance build-up with fentalogues, tolerance to phenomorphone develops slowly. It has the strong hedonic hallmarks of oxycodone/morphone, amplified many-fold, coupled w/ a mild-stimulating quality that leaves you feeling light, giddy, sunny-bunny, warm-fuzzy, and ready to conquer the world. It is especially attractive to users, such as the Duchess, who are not particularly affine to the highly sedating nature of certain opioids, such as diphenylpropylamines (methadone). N-(2-phenethyl)-noroxymorphone is not specifically listed as a controlled substance in the CSA or UN Conventions. Despite the potency and utility of phenomorphone and its N-arylalkyl cousins, it has received relatively little attention in the chemical-pharma literature and are also absent from the clandestine literature. Now armed with a simple, affordable and accessible route to noroxymorphone, it is my sincere hope that the RC opioid market will begin serious exploration of this uniquely euphoric niche of the opioverse.
For potency poachers, the 14-hydroxyl moiety on the morphinone nucleus is actually a more desirable target than N-substitution. For example, 14-Cinnamoyloxycodeinone, (14-cinnamoyloxycodone w/ the 7,8-double bond) has a very impressive analgesic potency ranging from 100 - 300 x morphine (I’ve found little relating its analgesic actiity to its potency as a euphoriant). The substitution of the 14-hydroxyl has been thoroughly explored and an SAR developed. Unlike the 14-hydroxyl, the N-arylalkyl analogues have received very little attention. This is likely due to the fact that further potency enhancements do not offer any clinical-therapeutic advantage over their N-methyl parents. This usually means that any potency gain in analgesia was coupled with increased addiction liability. Increased addiction liability almost always means increased euphoria. But for the clandestine community, who play the opio-potato sack race for the opposite reason, phenomorphone is a great place to get this party started.
Of course the Duchess would love to modify this beautiful molecule further. These ambitions include creating highly potent pairings of 14-phenylpropyloxy with various N-substituents suggested in the Helmut Schmidhammer article here: [
https://sci-hub.tw/10.1021/jm021118o]. The 3-OMe (3-methyl ether) analogues of naltrexone or naloxone would be ideal starting points for accessing some of these titillating compounds. The 3-OMe protection would allow selective 14-O-substitution and more straightforward access to the desired analogues. In the strange world of 14-phenylpropoxy analogues, N-allyl (naloxone) and N-CPM (naltrexone) substituents reign as the supreme agonists. This is absolutely bonkers. Along with a kick-ass name, Schmidhammer has been doing juicy things in the 4,5-epoxymorphinan arena, such as hammering out SARs on a series of potent metopon analogues and discovering this strange alternate dimension where N-allyl and N-CPM form agonists with an order of magnitude greater analgesic potency than their N-phenethyl siblings. While their full agonism, high analgesic activity, and lack of the expected antagonism would, logically, hint at some inherent euphoria, I am still skeptical of their potency as euphoriants relative to existing agonists, esp. their N-phenethyl cousins. When I first read the Schmindhammer study about a decade ago, I initially thought the deep hydrophobic binding pocket of the MOR, that which is accessed by the N-phenethyl residue of fentanyl, was being being finger-banged by the 14-phenylpropoxy substituent instead. While the N-allyl group was somehow working in a manner analogous to the 3-allyl function in allylprodine. I soon realized my mistake when reading about 14-Cinnamoyloxycodeinone and how the unsaturated allyl component of the 14-cinnamoyl moiety overlaid the 3-allyl residue in allylprodine, meaning that the opposite was likely true. The realities of this counterintuitive N-allyl/N-CPM interaction are likely due to the dynamic nature of ligand-receptor interaction. This interaction changes the 3D structure of its amino acid residues. The MOR has 400 residues. There is the phenomena of receptor heterogeneity to contend with as well as the up to 10 different MOR variant subtypes (indicated by sequencing). If inexpensive sources of the 3-methyl ethers of naltrexone and/or naloxone can be sourced, these would be very viable candidates for further investigation. Those wishing to go hog wild with further exploration into the euphoricopeia truffle-trove of 14-O-substitued-morphones are deserving of the highest of merit, including the distinct honor of (metaphorical? literal?) fellatio.
The primary goals of my extracurricular clandestine chemistry and monograph series are (a) to develop simplified straightforward syntheses of potent opioids that will be accessible to the hobbyist/clandestine community and (b) share my discoveries and experiences with the greater RC community. It’s the least I can do to help promote égalitarisme chimique: the chemically-modified egalitarianism of brain chemistry. We should all have the right [footnote #0] to pursue easily accessible pharmaceuticals that promote happiness. While phenomorphone has achieved the goal of a highly potent oxymorphone analogue accessible to the hobbyist/clandestine community via as few rxn steps as possible [N-deallylation of naloxone ---> oxymorphone + N-alkylation ---> phenomorphone], the work is never finished and forever in a state of flux. In fact, at this very moment, I’m hard at work on more surprises for my darling dearest bees, which is in addition to the numerous monographs that are in various states of progress, all of which are based on my personal experience with other opioid classes.
My interest in this convenient naloxone to noroxymorphone route emerged out of necessity: NPP shortages. A femme with a 300 mg/day Fabbit-Habit has quite the metaphorical feral feline on her back; a very hungry kitty indeed. These NPP droughts inspired this girl to discover not only alternative routes, but from the soil of necessity sprang forth brand new opio-sprouts. NPP once once imported with relative ease, but now that regulation places NPP importation under a tight squeeze, one must resort to a clever customs-circumvention trapeze, so in order to feed her dependencies, now that NPP no longer grows on trees, the Duchess must occasionally resort to an alternate main squeeze (If you wish to learn more about how to properly navigate the current Chinese regulatory/customs tight-rope, join the Opioid Den, or contact the Duchess directly via encrypted chat on Keybase, username: DuchessVonD ----> a lady never reveals ALL her secrets on the clearnet).
NPP may not grow on trees, but (in the USA at least) naloxone seems to be blooming everywhere, with every smiling panhandling politician and his mother handing out naloxone like smallpox blankets to the Indians as a solution to the opioid crisis. (“Try building a Tee-Pee out of N-allylnoroxymorphone, bitch!”) Seriously, naloxone is all over the place. It’s become a ubiquitous symbol of the opioid crisis. Let’s try to take full advantage of the Naloxone Bonanza while the getting is good.
When it comes to acquiring the requisite naloxone in practical quantities, this is not going to be achieved by visiting a pharmacy and purchasing a few mgs of the intranasal naloxone of commerce for $30. In the case of naloxone you should be thinking long-term and big picture: i.e. bulk importation. In order to meet increasing worldwide demand, production of this unregulated compound has never been greater. There are entire facilities (mostly in the Orient, aka: the land of the slanty-eyed jaundiced Manchurian munchkins) equipped for full-time production of naloxone in ridiculous quantities. Many are willing to part with kilograms of technical grade naloxone for prices that will surprise you and are deserving of some poetry:
Precious naloxo-cargo, doesn’t come from Japan,
So to Alibaba you go, with your sourcing plans,
To find a Chink, with which to shake his hands,
A technical grade discount, you must demand,
Narcan in the bush, is worth more once its lands,
