Indoles made simple by Canadian scientists
could greatly accelerate pharmaceutical production, while also
cutting costs and toxic by-products.
The reaction, designed by University of Toronto chemistry Professor Mark Lautens and graduate student Eric Fang, simplifies the creation of the basic molecular framework - an indole - found in many natural products and popular pharmaceuticals, including the multibillion dollar statin class of cholesterol-lowering drugs.
Until now, synthesizing this framework was inefficient, requiring six to 10 steps and often producing toxic by-products. "This new method only takes three steps and results in less waste," according to Lautens.
Indoles are ring structures containing carbon and nitrogen. In the new synthetic process, the researchers used a metallic element as a catalyst to form two chemical bonds and create a diverse range of indole-containing compounds. These compounds could be used to make drugs now on the market, or form the basis of new therapeutic drugs.
Lautens says this new molecular-level technique could equal big savings and less environmental impact. "In order to make a hundred kilograms of these best-selling drugs, there are often hundreds of litres of solvent used, not to mention the many purification processes involved. Not only are you speeding up the process, you're also reducing waste and energy used in manufacturing."
