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Cocaine, together with opium, cannabis and other less-common plant-based substances, has been used as a psychoactive substance for millennia. However, misuse of cocaine hydrochloride, which has been purified from Erythroxylum coca, its main natural source, originated in the early 20th century. Cocaine is under international control (Schedule I of the United Nations 1961 Convention; Class A in the MDAct). Although cocaine hydrochloride is normally insufflated to avoid destruction by digestive enzymes, conversion to ‘crack’, the free base, produces a smokable product. Because cocaine is widely available and its synthesis can prove challenging, there has been only limited interest amongst clandestine chemists in making either synthetic cocaine or in designing derivatives. A few so-called analogues of cocaine have appeared as illicit products, but some lack the tropane skeleton and are closer in structure to local anaesthetic drugs such as procaine which have no psychoactive properties.

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