Safer, cheaper building blocks for future anti-HIV and cancer drugs

July 3, 2014

A team of researchers from KU Leuven, in Belgium, has developed an economical, reliable and heavy metal-free chemical reaction that yields fully functional 1,2,3-triazoles. Triazoles are chemical compounds that can be used as building blocks for more complex chemical compounds, including pharmaceutical drugs.

Leveraging the compound's surprisingly stable structure, drug developers have successfully used 1,2,3-triazoles as in various anti-HIV, anti-cancer and anti-bacterial drugs. But efforts to synthesize the compound have been hampered by one serious hurdle: they depend on harmful heavy metals to work, and this severely limits their biological applications.

In new experiments reported in the journal Angewandte Chemie, Dr. Joice Thomas, Prof. Dr. Wim Dehaen and their team at KU Leuven's Molecular Design and Synthesis lab confirm for the first time that 1,2,3-triazoles can be synthesized through a metal-free, three-component reaction using readily available ingredients.

"We were able to develop a reaction that provided a good yield, high regioselectivity and easy access to diversely functionalized 1,2,3-triazoles," says corresponding author Prof. Dr. Wim Dehaen. "In other words, the reaction produces plenty of the compounds we're looking for, does so reliably without unwanted or unexpected outcomes, and does this in a way that makes it easy for us to isolate the compound. This makes our method highly desirable."

"Moving forward, we will focus on expanding the chemistry developed here to other new reactions while also exploring their possible applications in pharmaceutical as well as supra-molecular sciences," says lead author Dr. Joice Thomas.

Explore further: A bit of boron, a pinch of palladium: One-stop shop for the Suzuki reaction

Related Stories

Unexpected bond formation of chemical element boron

November 20, 2013

In synthetic chemistry, so-called element-element bonding can be systematically exploited to assemble small building blocks to obtain structures that are more complex than the "starting material" and can be used for the resource-saving ...

A breakthrough for organic reactions in water

June 26, 2014

Green-chemistry researchers at McGill University have discovered a way to use water as a solvent in one of the reactions most widely used to synthesize chemical products and pharmaceuticals.

Recommended for you

Force triggers gene expression by stretching chromatin

August 26, 2016

How genes in our DNA are expressed into traits within a cell is a complicated mystery with many players, the main suspects being chemical. However, a new study by University of Illinois researchers and collaborators in China ...

Isolation of Fe(IV) decamethylferrocene salts

August 29, 2016

(Phys.org)—Ferrocene is the model compound that students often learn when they are introduced to organometallic chemistry. It has an iron center that is coordinated to the π electrons in two cyclopentadienyl rings. (C5H5- ...

Bringing artificial enzymes closer to nature

August 29, 2016

Scientists at the University of Basel, ETH Zurich, and NCCR Molecular Systems Engineering have developed an artificial metalloenzyme that catalyses a reaction inside of cells without equivalent in nature. This could be a ...

0 comments

Please sign in to add a comment. Registration is free, and takes less than a minute. Read more

Click here to reset your password.
Sign in to get notified via email when new comments are made.