Community Research and Development Information Service - CORDIS

Periodic Report Summary 1 - CCT-MICROINDUS (Continuous Catalytic Transformations: from optimization in MICRO systems to INDustrial production)

In this project we develop new catalysts to operate under continuous flow conditions directly at the laboratory level. Design, preparation and first catalytic test integrate criterion of stability towards temperature and pressure as well as practical of continuous processes, clogging and pressure drop. The project thus clearly requires a multi-disciplinary approach involving chemistry, engineering, analytical and solid state expertise.
Of current problems faced by UCB Pharma, two main issues are addressed within the frame of this training and research program. Currently, two catalytic reactions are performed in batch mode leading to analogs of Levetiracetam, commercialized by UCB Pharma under the name of Keppra®.
The first goal of the project is to address the formation of a carbon carbon bond on a very electrodeficient heterocycle. The first approach based of a Mannich or a Friedel Craft reaction failed despite precedent in literature. Even homogeneous catalysts such as the triflic acid, sulfuric acid or any of the strongest Lewis acid did not promote the reaction. Alternative routes have therefore been evaluated though the construction of the aromatic ring at a late stage; finally some decent insight have recently been found using a copper mediated synthesis of a nitrile. We now expect to value this synthetic route in flow reactors.
The second goal of this project was to perform a stereoselective hydrogenation in flow systems. First catalysts were developed on the basis of the previous experience of University of Bordeaux. Supported nanoparticle showed eventually very good catalytic activities, and decent isomeric selectivity. Most of inorganic matrices common used in heterogeneous catalysis were screened and it turned out carbon was one of the best choices. The reaction proceeded smoothly at room temperature under atmospheric pressure of hydrogen leading to the target compound in nearly quantitative yields and sufficient purity. Alternatively we used lamellar composites in which we intercalated some metal salts. Satisfyingly, some of these composites led to improved selectivities. We then successfully implemented these metal modified catalysts in a small scale flow device.
The second part of the project will focus on finalizing the synthetic route for the heterocyclic compound and implementing both syntheses in flow systems in large scale in the industrial environment. This will eventually lead to the production of the Active Pharmaceutical Ingredient found in drugs using the CCT-Microindus techniques.

Contact person : Edith Norrant : edith.norrant@ucb.com

Reported by

UCB PHARMA SA
Belgium

Subjects

Life Sciences
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