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Metathesis
“A boon to organic synthetic chemists, olefin metathesis also promises cleaner, cheaper, and more efficient industrial processes” – A. Maureen Rouhi, C&EN Washington
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Pharmaceuticals |
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The $550B (5% growth) pharmaceutical industry develops new drugs to improve patient health. Developing pharmaceuticals is not simple or inexpensive; current estimates indicate that the average drug requires a commitment of over $1B before it reaches the market. The challenge continues after this point as price pressures and limited patent lifetimes ensure the window of opportunity is small and short. Tools that make early stage drug discovery and development easier or improve manufacturing margins are therefore in high demand.
Metathesis is such a tool. In drug discovery, Materia’s powerful technology is used to quickly synthesize novel compounds that would be difficult to produce using traditional synthetic methods.
In drug manufacturing, metathesis can be used to dramatically simplify synthetic processes. The technology can be used to reduce the number of steps, employ cheaper raw materials, and enable reactions without toxic solvents or unwanted by products. These benefits can dramatically reduce the overall cost of manufacturing.
Some examples of metathesis’ use in the pharmaceutical industry:
- Eisai Pharmaceuticals used metathesis in the discovery of a novel cancer drug. Eisai found that traditional synthetic techniques could not be used to produce the compound and metathesis was the only practical solution.
- Merck applied metathesis to quickly and efficiently produce the complex ring structures of its NK-1 receptor candidate. This spiro-system was synthesized in high yields from readily available starting materials.
- Boehringer Ingelheim produced over 400 kg of pharmaceutical material for their hepatitis C protease inhibitor program. This represents the largest amount of pharmaceutical material made using metathesis to date.
Nearly every major drug company and numerous pharmaceutically-focused academic groups use metathesis. The future will be bright as this intensive research translates into new drugs.
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