Re: On Methods Concerning the Synthesis of Opium

[Dilaudid]

"Dilaudid" <dda...@adelphia.net> wrote in message news:...
> Is this guy for real?
>
>
>
> On Methods Concerning the Synthesis of Opium
>
> David Allen Winne
>
>
>
>
>
>
>
> It is within the scope of vision to imagine a day when creation of
> medicinal
> compounds will be achieved stereochemically. This definition,
> "stereochemical" refers to a multifaceted, multidimensional derivation of
> molecular compounds through complex interactions inclusive of the entire
> components without first reducing them to their singular constituents. The
> purpose of this distinction is not to enhance the reader's comprehension
> of
> stereochemistry rather to demonstrate the author understands the
> similarities and digressions outlined within the discipline of
> stereochemistry as defined1 and the proposal identified herein. Although
> such medicinal advances remain imaginable, there is no proposed suggestion
> as to when accomplished derivatives of this methodology will finally see
> complete fruition.
>
>
>
> Alkaloids derived through analysis of opium have been quantized and
> isolated to their singular components. Leaving the most potent analgesic
> derived as diacetylmorphine (excluding etorphine etc.derived from
> oripavine,
> which is also a secondary transformation). It does not take a stretch of
> imagination to draw the conclusion that acetylation of morphine base with
> acetic acid instead of acetic anhydride will yield monoacetylmorphine (in
> the alcoholic 6-hydroxyl group). This conclusion was immediately prevalent
> when first reviewing the structure of diacetylmorphine. It also was not an
> original conclusion as shown below.
>
>
>
> "6-monoacetylmorphine already has a free 3-hydroxy group and shares
> the high lipophilicity of heroin, so it penetrates the brain just as
> quickly
> and does not need to be deacetylated at the 3-position in order to be
> bioactivated; this makes 6-monoacetylmorphine somewhat more potent than
> heroin, but it is rarely encountered as an illicit drug due to the
> difficulty in selectively acetylating morphine at the 6-position without
> also acetylating the 3-position. This can however be accomplished by using
> acetic acid with an appropriate catalyst to carry out the acetylation,
> rather than acetic anhydride, as acetic acid is not a strong enough
> acetylating agent to acetylate the phenolic 3-hydroxy group but is able to
> acetylate the 6-hydroxy group, thus selectively producing 6-MAM rather
> than
> heroin."(http://en.wikipedia.org/wiki/Monoacetylmorphine).
>
>
>
> Considering an objective to obtain opiate derivatives through
> acetylation of raw opium, stochastically deriving potent analogs, without
> first isolating the constituent components, a reasonable analogy being the
> process of learning to play a musical instrument, the student must at
> first
> learn to identify single notes (and fractions thereof), then scales, and
> finally chords. Through years of study and instruction, the student may
> then
> choose which notes fall into harmonious or dissonant conclusions within
> the
> musical piece being created. Notably, the most colorful passages of a
> piece
> being assembled from the synthesis of notes falling within as well as
> without the prospective scales inside the structure of the key of the
> piece
> of music, it is these "blue" notes that create the very essence of the
> artistic effort, through emotions of the author. Within the strictest
> confines of the theory and application, these notes may not fit, however,
> without them the piece is reduced once again to a mere scale devoid of
> artistic emphasis or import. Such is the nature of all great human
> endeavors.
>
>
>
> To great benefit, years of effort have been put forth obtaining and
> reducing compounds to their lowest common denominators by isolating
> important discoveries and enabling humankind to grasp the building blocks
> of
> molecular compounds. The process requires this most tedious and devoted
> effort to isolate and identify interactions at their very basic
> fundamental
> level. Chemicals such as morphine, codeine, hydrocodone, hydromorphone,
> and
> so on, have provided incalculable benefit to the human species.
> Additionally, the process may through necessity continue unabated over the
> next several hundred years only to find completion upon exhaustion of all
> potential isolations and reductions available. This leaves the origin of
> chemical analysis in its infancy at present just beginning to crawl and
> upon
> mastery then to begin walking prior to a steady run. Once again to begin
> recombination of essential singular molecular compounds one by one until
> all
> necessary derivatives have been catalogued a second time over. The final
> arrival at stereochemical projection of complex molecular compounds
> recombining in a quaternary synergy only obtained through
> three-dimensional
> interactions intrinsically integral to the unique recombination of the
> original complex molecular compounds themselves a fingerprint unique
> specifically to each individual synergistic interaction.
>
>
>
> Diacetylmorphine in and of itself appears a stereochemical compound
> with the acetylation of morphine base with acetic anhydride creating two
> isomers of monoacetylmorphine. This synthesis does not appear synergistic,
> for example, a chemical compound expressing a synergistic effect would be
> hydrocodone mixed with aspirin (or acetaminophen). The synthesis of the
> two
> compounds creates a synergistic effect elevating the strength through
> lesser
> amounts of either component (although not stereochemical). This does not
> have any relevance upon the stereochemical composition of diacetylmorphine
> merely that the "di"-acetylation synthesis bears no significant
> synergistic
> contribution (and is likely accidental). This distinction is critical in
> relation to this papers definition given for stereochemistry. The
> stereochemical composition of diacetylmorphine with the necessary
> inclusion
> of two isomers of 3-monoacetylmorphine and 6-monoacetylmorphine yields the
> appropriate non-reactive isomer 3-monoacetylmorphine as a chiral
> counterpart
> to the reactive 6-monoacetylmorphine. This is congruent to the acetic
> anhydride molecules mirror-like stereo projection of two acetic acid
> molecules prior to the acetylation of morphine base into diacetylmorphine.
> While the interrelationship of the chemistry outlined is consistent with
> the
> classical definition of stereochemistry. It digresses for clarity of
> purpose
> when understanding proposed methodology, the indicated method herein being
> a
> "stereochemical" approach to stereochemistry. A quaternary enterprise
> entertaining the process of visualizing the entire molecular compound from
> every direction at once as well as attempting to parallel isomers with
> chiral counterparts and potential inclusion of racemization of one
> enantiomer into another.
>
>
>
> The intent and purpose of synthesizing complex molecular compounds in
> one transition is to obtain the additional benefit of a multidimensional
> synthesis as outlined above. Taking advantage of one molecular transition
> as
> well as the additional benefit of a second transition only available due
> to
> the complex molecular compound and the state of flux created upon the
> initial transition phase. This enables a molecular transition unseen in
> simple compound composition due to the absence of multiple molecular
> transitions being available. Not only does the complex molecular compound
> transform but also as it is transforming, the state of transition opens
> opportunities for additional molecular transitions unforeseen in any
> simple
> molecular compound transaction. This effectively creates limitless
> potential
> parameters for the accumulation of medicinal compounds. The actual limit
> is
> defined by the ability of the human being to predict and derive the
> necessary transitions required and attempt to verify them through
> experimentation. It is as the three-body problem in classical physics,
> anything beyond becomes too difficult to calculate in terms of obtaining a
> useful result.
>
>
>
> Returning once again to our musical analogy, scales comprised of
> specific root notes retain both their major and minor properties enabling
> entirely different moods to become prevalent by mere redesignation of the
> root note. Taking this to its furthest extent enables modal use of scales
> thereby creating twelve uniquely different scalar functions through the
> alternative assignment of root notes. Hence, Aeolian, Ionian, Phrygian,
> Lydian, Mixolydian, and Dorian modes etc.are derived from one scale at
> numerous root positions. This very same modal composition can be applied
> to
> any molecular compound thereby deriving several different components with
> unique properties by simply manipulating the key atom in the root
> position.
> This can go on indefinitely without end effectively creating a "harmony of
> the spheres" sufficient to roll Johannes Kepler in his grave.
>
>
>
> Additionally, in congruence with musical analogy is the necessary
> inclusion of harmonic, tonic, and diatonic triad inversions equating to
> the
> chemical conversion of a single molecular compound into a stereochemical
> product. The result includes the necessary construction of "Chords" the
> musical equivalent of "stereochemically" doing stereochemistry.
>
>
>
> Effectively, the result is working with complex molecular compounds
> attempting to synthesize key components within, three-dimensionally,
> remains
> the equivalent, of chord building technology in music theory. Naturally
> imagining a musical product entirely devoid of chords is the equivalent of
> investigating modern advances in chemistry. We are at the scale and note
> building phase of the industry. Only time can tell when medicines derived
> from chorale counterparts becomes available. Certainly, anyone can pick up
> a
> pile of pills, swallow them, and experience several diverse effects (both
> good and bad). This is exactly why it will take so long to accomplish the
> necessary analysis and understanding of chemical compounds. Very few
> people
> would appreciate the consequences of such activity necessitating
> appropriate
> precautions in effect in current study of molecular compounds.
>
>
>
> The inclusion of all opium alkaloids creates circumstances both
> complimentary and contradictory in nature imparting a synergy not apparent
> through isolation of specific compounds, metabolites, or isomers. The
> author
> makes no pretense in the assumption that synergistic compounds will be
> produced through the intended approach; merely that it is a distant-future
> possibility. A possibility that awaits progress obtained only through
> diligent isolation of endless singular molecular compounds and
> recombination
> of those compounds with endless others developing a broad enough
> foundation
> to begin contemplation of elevated synthesis of complex molecular
> compounds.
>
>
>
> Summary:
>
>
>
> The purpose behind the approach envisioned is summarized through
> experiences related to the administration of pharmaceutical compounds
> derived and isolated from opium alkaloids. Examples such as hydrocodone,
> morphine, codeine, and oxycodone all have limited useful parameters such
> as
> fast onset with short duration or limited (not to be confused with potent)
> psychoactive properties in comparison to simple opium extract containing
> the
> entire spectrum of alkaloids.
>
>
>
> In addition, the after effects of any of these pharmaceuticals leave
> one feeling "strung out" or "hung over" in comparison to basic opium
> extract. A large degree of this feeling is attributed to some of the
> additive ingredients typically associated with some opiates such as
> acetaminophen, aspirin, etc.However; the entire effect is not attributable
> to the additives. Moreover, extensive analysis of the properties of these
> isolated compounds derived for medicinal use tends to leave the impression
> (rightfully so) of specific medicinal focus. Specifically, they tend to
> hit
> hard and taper off fast opposed to a slower onset with longer duration.
>
>
>
> The experience increases in proportion to use of these pharmaceuticals
> adjunct to pure opium extracts. I.e. using opium extracts daily then
> switching over to pharmaceuticals conveys an effective sense of the
> limitations imposed through isolation of specific alkaloids. An analogy
> would be suggesting that one took morphine, codeine, and thebaine
> (hydrocodone, acetyldihydrocodeine, oxycodone, and oxymorphone) all at
> once.
> It readily becomes evident exactly how strong and effective opium is with
> its complete compliment of alkaloids. However, the effects of the pure
> opium
> extract are subtle as well as powerful and the observed onset of analgesia
> is decidedly weak in comparison to certain isolated derivatives above.
>
>
>
> It is with this observation that an attempt to synthesize constituent
> components included within opium, eliminating certain intermediary
> transitions is intended to satisfy potential objectives otherwise
> accomplished through isolation of specific compounds. Notably, acetylating
> the 6-hydroxyl group in morphine alone will sufficiently amplify the
> pharmacological effects of raw opium. Additionally, the extraction and
> isolation of compounds such as morphine from opium derived from dried
> poppy
> pods becomes somewhat pointless since the overall effect of the product is
> generally stronger and less time consuming. It merely is not as analgesic
> as
> the isolated compounds (this is due largely in part to the degree of
> consumption) when taken in concentration.
>
>
>
> Method:
>
>
>
> The first time the author-extracted alkaloids from the opium poppy, a
> container of extract decanted from dried, ground pods placed within an
> Espresso machine and run through with a solution of 5% acetic acid. The
> solution obtained therein placed upon a burner and simmered slowly until
> all
> evidence of liquid evaporated. The crystalline residue obtained by
> scraping
> the sides of the container ignited within a pipe leaving the author
> feeling
> happy and well disposed. Upon this occasion, no substantial quantity of
> material was derived to investigate additional properties therein. It is
> noted that this author knew nothing regarding the chemistry of opium at
> the
> time and was merely looking for a more effective way to extract tea from
> poppies.
>
>
>
> On the second occasion this method was conducted, only stems from the
> Papaver Sominiferum species were used and twelve cups of a solution of 5%
> acetic acid were decanted from a coffee maker (run through twice).
> Approximately 1.5 cups (dry measure) of poppy straw was used. The solution
> was then placed upon a burner to slow simmer until distillation
> substantially reduced the quantity of liquid therein (approximately three
> hours). The entire solution was then relocated to a three-cup pot
> (extremely
> small) to simmer over night. Upon examination, the next day the ½-inch
> solution had evaporated to less than a 1/8-inch across the bottom with
> crystalline deposits from the ½-inch mark to the top of the solution. Into
> this solution was introduced approximately 15 ml of hydrochloric acid with
> no apparent reaction. Then approximately ½ teaspoon of bicarbonate of soda
> was added to the mixture causing the entire pot to foam for about ten
> minutes. Soon thereafter, introducing a small round brush (made of
> horsehair) into the liquid rapidly stirring caused the mixture to die down
> to a viscous state.
>
>
>
> Letting the pot sit for about ten minutes, the author then began
> rotating the pot twisting the liquid at a 45-degree angle thereby causing
> the liquid to rise upon the walls evaporating rapidly and quickly becoming
> a
> uniform paste. The pot was then cooled while the paste was obtained upon a
> small putty knife, (the material collected amounted to approximately a
> teaspoon). In addition to the Brown paste-like substance, was a hard
> crystalline deposit along the bottom ½ inch of the side of the pot (it is
> likely that the paste would have become crystalline if left undisturbed).
> This material was chipped away yielding a thimble full of material. The
> material placed within a pipe and smoked left some small effect upon the
> subject. The additional consumption of four pea-size rolled balls of paste
> left the author with exceptional sensitivity to light and some
> urine-retention effects. Compounding this feeling was a definite
> "opiate-like" state however, the extent of the effects are largely lost
> upon
> the author's tolerance for opiates. In addition, the degree of morphine
> within the sample is highly suspect since the sample was accumulated from
> poppy straw instead of poppy pods, which is the usual part kept for the
> extraction.
>
>
>
> Hypothesis:
>
>
>
> The use of acetic acid when acetylating morphine base creates
> 6-monoacetylmorphine. There is no point with present day knowledge to
> obtain
> Diacetylmorphine for licit or illicit purposes. The only active
> metabolites
> derived from the process are 6-monoacetylmorphine, and morphine. These
> metabolites obtained without the additional step of creating
> Diacetylmorphine alleviate the body's metabolism from deacetylation of the
> 3-hydroxyl group maintaining equivalent pharmacological results.
>
>
>
> Extending this application to opium extract decanted from poppy pods
> with a solution of 5% acetic acid effectively acetylating the 6-hydroxyl
> group in morphine alone will sufficiently amplify the pharmacological
> effects of raw opium thereby creating a more bioavailable compound for
> use.
> There remains the additional possibility of a phase transition enabling
> additional alkaloids to become transformed. It remains uncertain if this
> additional transition will be synergistic or beneficial to the overall
> product. This
>
> "extract" tea from poppies process excludes the possibility of injectable
> medicinal value without the inclusion of a cleansing and purification
> stage.
>
>
>
> "According to Small and Lutz in The Chemistry of the Opium Alkaloids,
> a
> report commissioned by the U.S. Public Health Service in 1932, "when
> morphine is heated with acetic anhydride two acetyl derivatives are
> formed;
> [alpha]-acetylmorphine and ß-acetylmorphine probably have respectively the
> phenolic and alcoholic hydroxyl groups acetylated." That is,
> [alpha]-acetylmorphine is 3-monoacetylmorphine (3-MAM) and
> ß-acetylmorphine
> is 6-monoacetylmorphine (6-MAM)."
>
>
>
>
>
>
>
> [On the Action of Organic Acids and their Anhydrides on the Natural
> Alkaloids. C.R.A. Wright, D.Sc., Lecturer on Chemistry, St. Mary's
> Hospital
> Medical School, London. (Journal of The Chemical Society, Vol. 27 (1874),
> pp. 1031-1043.)]
>
>
>
> Conclusion:
>
>
>
> One of the most significant advances in modern medicine in the
> nineteenth century was the stereochemical synthesis of diacetylmorphine
> from
> morphine. This is clearly demonstrated by the relative order of magnitude
> increase in the strength of the final product. The fact that the greater
> majority of modern medical institutions elect to leave this solution out
> as
> an analgesic choice for their patients serves as tacit confirmation of the
> significance of stereochemical product strength.
>
>
>
> While this fact may be evident in the case of diacetylmorphine, the
> real objective is to obtain moderate synergistic effects from complex
> molecular compounds through enhancement of existing properties of their
> alkaloid origin. This selective method hopes to enhance the effective
> properties of the chemistry without losing the inherent natural basis of
> origin. The summary of contents in chemical analysis in this approach
> hopes
> to accomplish greater results with less of the side effects that plague
> methodologies using isolation and reduction tactics.
>
>
>
> Isolating diacetylmorphine from its parental alkaloid group strips it
> of any redeeming properties found within the other constituents. This
> fundamental failure contributes to its overwhelming success in the
> strength
> category while stigmatizing its benefit with the addictive stigma that may
> have otherwise been avoided had the entire alkaloids properties been
> retained. This is not intended to suggest that addictive properties would
> no
> longer be present merely that they may not have been magnified to such
> great
> extent with additional opposing alkaloid components.
>
>
>
> 1. "Stereochemistry, a subdiscipline of chemistry, involves the study of
> the
> relative spatial arrangement of atoms within molecules. An important
> branch
> of stereochemistry is the study of chiral molecules,"
> http://en.wikipedia.org/wiki/Stereochemistry
>
>
>
>

[Spencer Spindrift]

I have been fortunate to have had some raw, unprocessed opium once in my
life. I have also tried the derivatives and the synthetic analogues.
IMHO raw unprocessed opium is much better as well as being safer to use.
As there is more opium in Afganistan than they know what to do with, it
would make sense to reclassify opium as a soft drug so people would not
find heroin first and become junkies. Unfortunately this is not going to
happen.

I am not much good at growing plants but have successfully cultivated
pot a couple of times.

I once bought a small opium poppy plant in a pot but it failed to grow
and soon died. I don't think it would be difficult to home grow opium if
you knew how to do it. Also there is some opium in common or garden
poppies so what is the point of all this complex chemistry?