New method facilitates the construction of medicines
Researchers at the University of Gothenburg have discovered a new method for building compounds with halogens, which are included in most medicines. The method is more efficient and cheaper than those used today.
During drug manufacturing, new chemical compounds are built that can interact with the body in different ways. Often halogens, such as chlorine, bromine or iodine, are used as handles to connect several molecules. But the chemists have struggled to get the halogens to stick in the right place in the molecule without destroying important properties in the process.
“The traditional methods often result in complicated mixtures of products and require complex reaction conditions. But now we have found a shortcut in this complex world,” says Henrik Sundén, researcher at the University of Gothenburg and lead author of the study published in Chemical Science.
Utilizes the reactivity of the boron atom
Henrik Sundén's team has come up with a way to take advantage of the reactivity of the boron atom, which makes the binding of halogens to molecules more efficient and feasible. When designing drugs, researchers often start from modified benzene rings (aryl amides), and by first creating a reaction with boron, it becomes easier to attach a halogen to the molecule, without the molecule being at risk of deterioration. These molecules serve as building blocks for many important compounds, especially in medicinal chemistry.
“The halogens don't just work as good handles to connect molecules. The halogen can also be important for a compound's biological activity. That is, a halogen in the right place can determine whether a molecule gets the right properties required to ultimately become a medicine,” explains Henrik Sundén.
The researchers' method simplifies the process and also opens up exciting possibilities for a more efficient and scalable production of compounds with significant applications in areas such as medicine and materials science. The group that developed the method also includes researchers from Chalmers and Astra Zeneca.
“The discovery is a good example of how basic scientific innovation can lead to practical solutions for real challenges,” says Henrik Sundén.
Scientific article in Chemical Science: Regioselective Ortho Halogenation of N-Aryl Amides and Ureas via Oxidative Halodeboronation: Harnessing Boron Reactivity for Efficient C-Halogen Bond Installation
Contact: Henrik Sundén, researcher in organic chemistry at the Department of Chemistry and Molecular Biology at the University of Gothenburg, telephone: 0708-92 46 71, e-mail: henrik.sunden@chem.gu.se