TOP grant for one-pot syntheses

Professor Romano Orru of the Synthetic & Bio-Organic Chemistry research group has been awarded a TOP grant of €780.000 by the Netherlands Organization for Scientific Research (NWO). The funding enables him and assistant professor Eelco Ruijter to strengthen their research line on the production of drug-like molecules with novel and ultra-short one-pot synthetic routes.

05/09/2014 | 4:17 PM

The development and production of pharmaceuticals consumes large quantities of natural resources and is often far from sustainable. Especially the production of complex bio-active molecules and active pharmaceutical ingredients are energy consuming and involves waste of solvents and separation agents. It is therefore crucial to design and develop sustainable synthetic manufacturing processes. Professor Orru: “We believe that using less toxic and more common reagents and catalysts such as enzymes improves the eco-balance in pharmaceutical manufacturing.”

Enhancing chemical yield
The Synthetic & Bio-Organic Chemistry research group, embedded in the Department of Chemistry & Pharmaceutical Sciences and the Amsterdam Institute for Molecules, Medicines and Systems combines enzymes and other green synthetic methodologies with so-called one-pot processes: successive chemical reactions in one reactor. This strategy reduces the formation of by-products and enhances the chemical yield.

Using this methodology, the group developed a very short synthetic route for telaprevir: the leading drug against hepatitis C. Worldwide, over 200 million people suffer from this chronic infectious liver disease. The synthesis was reported and patented in 2010 and has been scaled to multi-kilogram production. Manufacturing on industrial scale is currently under development.

Romano Orru   Eelco Ruijter

Prof. dr. Romano Orru and Dr. Eelco Ruijter of the Synthetic & Bio-Organic Chemistry research group receive a TOP grant of €780.000 from NWO to strengthen their research line on one-pot syntheses.

The group works on multicomponent and one-pot syntheses since 2003. The researchers apply these methods to the diversity-oriented synthesis of fine chemicals with a high added value, like building blocks for medicines or ligands for catalysis. The awarded TOP grant enables funding for three PhD projects and expansion of laboratory equipment. Orru enthusiastically claims: “This is exciting research. The PhD students in this project will work in a stimulating and challenging environment and will receive top training in synthetic chemistry of the 21st century.” 

About NWO TOP grant
NWO awards TOP grants in chemical sciences annually to excellent and established research groups with a clear chemical, biochemical or chemical-technological reputation. The research group uses the grant to strengthen or renew challenging and innovative research lines. NWO granted only 5 of the 31 chemical sciences applications this year.

More information
Key publication 1: A highly efficient synthesis of telaprevir by strategic use of biocatalysis and multicomponent reactions

Key publication 2: Highly stereoselective synthesis of substituted prolyl peptides using a combination of biocatalytic desymmetrization and multicomponent reactions

Synthetic & Bio-Organic Chemistry research group