Australasian Science: Australia's authority on science since 1938

Lab Accident Cuts the Cost of Addiction Drugs

By Stephen Luntz

A laboratory accident has shown the way to cheaper production of opiates used to treat heroin and alcohol addiction.

In an event that echoes Alexander Fleming’s discovery of penicillin, a laboratory accident has shown the way to cheaper production of opiates used to treat heroin and alcohol addiction.

“It was quite a fortuitous discovery,” says Prof Peter Scammells of the Monash Institute of Pharmaceutical Sciences. “One night, quite by accident, a member of our group left a stainless steel spatula in her reaction. In the morning we found a high amount of the desired product in the flask. Since then we have been raiding the Institute’s stationery cupboard for cheap stainless steel paper clips!”

The production of buprenorphine and naltrexone requires several steps, including the removal of a methyl group from the nitrogen atom in morphine extracted from opium poppies. This is generally conducted using cyanogen–bromide, a toxic chemical that Scammells says “doesn’t always give good yields, particularly on a large scale”.

Other techniques have been tried, but all have their problems; while other stages in the process have been optimised, the methyl group’s removal has become the limiting step.

Scammells says that since the discovery the team has investigated how steel facilitates the reaction. “We think it is acting as a catalyst in a redox reaction, but we’re still working on this.”

Having decided that the use of paper clips was somewhat unscientific, the researchers tested raw iron and various grades of stainless steel. “We found that iron has a slightly different selectivity from stainless steel, so different reactions are suited to different catalysts. We’ve patented the process with both,” Scammells says.

In Australia, buprenorphine and naltrexone are only used to treat opiate and alcohol addictions, but Scammells says that buprenorphine is licensed in Europe as an analgesic with fewer side-effects and less chance of addiction than morphine.

He thinks it is possible the discovery, published in Organic Biomolecular Chemistry, will open the drugs up for wider use now that prices will fall.