Cocaine analogues for sale


Cocaine analogues have substituents at positions 2 and 3 of the trochanic nucleus. They are contained in leaves of coca bush in the amount about 1% (cultivated plants contain them significantly less). Synthetic cocaine analogs are colorless bitter taste crystals with a melting point -15.8°C (in water), readily soluble in water and ethanol. When acidic or alkaline hydrolysis decomposes into benzoic acid, methanol and ecgonine. In industry, cocaine is obtained by extraction from coca leaves or by saponification of a alkaloids mixture to the ecgonine, followed by methylation of its carboxyl group and benzoylation. After it was found that cocaine is a benzoylecgonine methyl ester, attempts were made to implement a partial synthesis of cocaine analogues, i.e. get cocaine back from the ecgonine, which is the product of decay. This question had great practical importance. Leaves of coca contain few cocaine analogues and a lot of cinnamyl cocaine. Since the latter, by its pharmacological properties is much inferior to cocaine, it was desirable to turn it into a more valuable product. In addition, during the raw cocaine purification, a rather significant amount of contaminated residues departs, which it was also desirable to use. In view of the fact that cinnamyl cocaine give the same ecgonine in hydrolysis as cocaine itself, it is clear that synthesis of cocaine from the ecgonine solved both questions immediately: by hydrolyzing a mixture of low-value alkaloids and transferring the ecgonine resulting to cocaine, we, in the final analysis , we can get more cocaine than it was originally in the plant. This was particularly beneficial at a time when the coca leaf price was determined based on the content of cocaine found by the analysis. This particular legal cocaine analogues synthesis presents no difficulties and can be carried out in two variants, which are classical reactions application of benzoylation and esterification. In the first variant, the ecgonine is first esterified by heating with methyl alcohol and gaseous hydrochloric acid. The methylecgonine obtained is benzoylated by heating with benzoyl chloride or with a benzoic acid and POCl3 mixture. In a second variant, the ecgonine is first benzoylated by heating with benzoic anhydride, and the benzoylecgonine thus obtained is then esterified with either methyl iodide or dimethyl sulphate. The complete cocaine synthesis was carried out by Willstatter, starting from the tropinone. Under the metallic sodium and carbon dioxide action on tropinone, tropinone-B-carboxylic acid is formed (along with other products). When it is restored, a small amount of ectonine is formed, which, as we have seen, can be converted into cocaine. This synthesis has only a purely theoretical interest.

Pharmacological effects

Cocaine and its synthetic analogues block the nerve impulses conduct and have a local vasoconstrictor effect, reducing the norepinephrine reuptake. Due to the high toxicity and ability to cause dependence, this research chemical has gradually disappeared from use. Its toxicity is due to catecholamines reuptake inhibition, both in the peripheral and central nervous system. Violation of this capture in CNS synapses  is also explained by cocaine-induced euphoria. Currently, cocaine is used only for superficial anesthesia of the upper respiratory tract, allowing simultaneous anesthesia, vasoconstriction, and mucosa swelling. Cocaine hydrochloride is used in the form of 1,4 or 10% solution for topical application. To reduce side effects in most cases, apply 1 or 4% solution. The cocaine and its analogs reinforcing effect is largely due to the ability of these substances to inhibit dopamine reuptake. As a result, dopamine receptors stimulation in different parts of the brain is intensified. It also blocks the norepinephrine and serotonin reuptake, and so, over time, adrenergic and serotonergic brain systems develop. This is evidenced by a decrease in the corresponding metabolites content: 3.4-dihydroxyphenylethylene glycol (noradrenaline metabolite) and 5-hydroxyindoleacetic acid (a metabolite of serotonin). Cocaine and its analogues cause a dose-dependent increase in heart rate and blood pressure, increases overall activity, improves performance of tasks requiring attention and reaction. In addition, cocaine causes a self-confidence sense and a well-being sense. Higher doses lead to euphoria. The latter does not last long and often prompts taking cocaine again. At repeated introduction possible involuntary actions, stereotypic behavior and delirium. Long-abusing cocaine makes irritable and aggressive.


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