New Class of Stable and Easy-to-Use Boron Compounds Developed

A research team at the University of Gothenburg has introduced a new class of boron-fluorine compounds that could simplify and improve drug development. These compounds, known as BF₂‑boracycles, allow scientists to enhance a medicine’s effect or reduce its side effects without dismantling its structure.

Boron-based molecules are essential tools in modern chemistry, used in producing pharmaceuticals, advanced materials, and diagnostic agents. However, synthesizing boron compounds that position the boron atom precisely within a complex molecule has remained difficult. This challenge has limited opportunities for modifying existing drugs or bioactive substances.

“In our study, we have developed a new class of stable and easy‑to‑use boron compounds, known as BF₂‑boracycles. These can be produced in a simple, metal‑free, and scalable way without time‑consuming purification steps,” says Henrik Sundén, senior author on the paper published in Angewandte Chemie. The compounds combine unusual stability with high reactivity, allowing chemists to modify finished molecules at a late stage. This capability means a completed drug or biologically active substance can be adjusted to improve its properties without reconstruction from scratch.

Compared with existing synthesis routes, the new method reduces the number of steps, decreases chemical waste, and increases resource efficiency, contributing to more sustainable drug design. The development involved collaboration with the University of Caen in France and the University of Ljubljana in Slovenia, as well as partnership with AstraZeneca.

The key reaction replaces a hydrogen atom in a drug molecule with the newly developed boron compound. That boron compound can then be exchanged for another molecule that provides the desired improvement. As Sundén notes, “Our discovery means that you don't have to take the drug apart to improve it. Instead, you can test perhaps a hundred different functional molecules that easily replace the boron compound to see which molecule best improves the drug.”

The study also shows that these boron compounds can substitute for various chemical groups, such as halogens, alcohols, and azides, and can incorporate radioactive iodine—an element crucial for cancer diagnosis. This versatility extends the method’s potential to both drug refinement and medical imaging.