"We took small molecules and clipped them together like Lego," said lead researcher Professor Michael Sherburn, from the Research School of Chemistry.
"The building blocks are carefully designed in such a way that the first reaction generates a product perfectly primed for the second. It's quite magical. This means you can efficiently build large and complex molecules."
Medicines of this type have traditionally been made in a cumbersome way. Chemists take a related molecule and renovate it. This is a lengthy process, with unwanted structural features being ripped out and replaced.
"This leads to a lot of waste," Professor Sherburn said.
The group trialed their innovative new method by making pseudopterosin, a powerful anti-inflammatory and analgesic drug, which is currently only available in tiny quantities extracted from fan coral found in the Bahamas.
The work began as blue-sky research, with the researchers trying to work out a way to make supposedly impossible molecules of cross-conjugated hydrocarbons.
Before trying the experiments the team ran simulations on the Raijin supercomputer, which indicated that their method had potential.
"Ours is an empowering and enabling technique, allowing a smarter and faster way to make important substances," said Dr Chris Newton, who did the research in the laboratory as a PhD student.
"The pseudopterosin synthesis is the tip of the iceberg. We are well on the way to efficient syntheses of other important drugs.
"There is a potential for industrial-scale manufacture, too, which will take the pressure off species which are being harvested for drugs," he said.
The research is published in Nature Chemistry, doi:10.1038/nchem.2112