Fast and cheap
Scientists have proposed a simple and effective method for obtaining water-soluble fullerene compounds for use in medicine.
Fullerenes C 60 and C 70 are an unusual molecular form of carbon. Depending on the number of atoms in the molecule, fullerenes resemble a football (with 60) or a rugby ball (with 70) in shape. Compounds based on fullerenes have long been considered a promising basis for the creation of new medicines due to their pronounced antiviral, antibacterial, antitumor and antioxidant activity.
Unfortunately, fullerenes themselves are absolutely insoluble in water, which prevents their use in medicine. The currently existing classical methods for the synthesis of water-soluble compounds directly from fullerenes allow them to be obtained only with a small yield (usually up to 10%) in several complex synthetic stages. These methods are not applicable for the industrial synthesis of water-soluble fullerene compounds, which makes it extremely difficult to create medicines based on them.
The research group led by Pavel Troshin, Professor at the Skoltech Center for Energy Technologies, has extensive experience in the synthesis of water-soluble fullerene derivatives. In their latest work, scientists have proposed an effective one-step method for obtaining stable water-soluble fullerene derivatives with high activity against human immunodeficiency virus (HIV).
The work was published in the journal Chemical Communications (Kraevaya et al., Direct arylation of C 60 Cl 6 and C 70 Cl 8 with carboxylic acids: a synthetic avenue to water-soluble fullerene derivatives with promising antiviral activity) and announced on its cover.
The developed method makes it possible to obtain these compounds with a yield close to 100% without lengthy and time-consuming chromatographic purification, which opens up new opportunities for the synthesis of fullerene derivatives at any scale required for the pharmaceutical industry.
Figure from the article Kraevaya et al. – VM.
"Despite the fact that more than 20 years have passed since the discovery of the high antiviral activity of fullerene derivatives, these unique compounds remained unavailable for clinical trials, since their preparation turned out to be very time-consuming. We hope that our proposed simple and one–step method for the synthesis of water-soluble fullerene compounds will solve this problem and bring us one step closer to creating effective antiviral drugs based on them," says the first author of the published work, graduate student Olga Kraevaya.
The results obtained in the framework of the work open up new opportunities for the targeted design of water-soluble fullerene derivatives with a given set of properties, which in the future will allow the introduction of a new generation of drugs based on these compounds to the market.
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