NovProCat2: Novos Processos Catalíticos e Catalisadores para a obtenção de Fármacos

Chiral amines are present in many important drugs, particularly those for treating flu, diabetes, Alzheimer's (AD) and Parkinson disease and lowering cholesterol. In the case of AD, worldwide there are 35 million people with the disease and this number is expected to increase 3 to 4 times until 2050. No cure exists and this is actually costing the world €400 billion. In the Alentejo, where there is a significant ageing population, AD is a very serious problem. 45% of molecules that chemists are developing into drugs contain a chiral amine unit well known examples include: rivastagimine, rasagline, sertraline and indatraline etc. Chiral amine containing drugs have a market volume of millions of euros. Dibenzodiazapines (DBDAs) are a family of compounds that have important medicinal properties, many of which are used in the treatment of depression or schizophrenia, or used as a tranquilizer. The market for these drugs is worth billions of euros. Industrially, chiral amines are obtained via imine hydrogenation this process is expensive and hazardous. Hydrosilylation is an alternative method for transforming ketimines to chiral amines. Organocatalysts can be successfully used. Organocatalytic methods have become recently industrially attractive, as they are free of toxic metals, and can be run in air and water. We have currently a US patent granted for this novel catalyst and process that give chiral amines (US9844773) and a European patent in progress (EP3055062 (A1)).

In the case of the technology leading to the DBDA products, we have two international patents that have been published and are in an advanced state: US2018105502 and EP3310765 (A1)).