High Throughput Screening and Evolution of a Library of Ligands in Asymmetric H-Transfer Reduction of Acetophenone

Title: High Throughput Screening and Evolution of a Library of Ligands in Asymmetric H-Transfer Reduction of Acetophenone

Volume: 13 Issue: 5

Author(s): Radwan Abdallah, Pierre Grenouillet, Nicolas Vriamont, Olivier Riant and Claude de Bellefon

Affiliation:

Keywords: Homogeneous catalysis, high throughput screening, combinatorial catalysis, ligand library, asymmetric hydrogenation

Abstract: A library of 117 ligands was combined with three transition metals Ru, Rh and Ir and screened with three different operating conditions for the asymmetric H-transfer reduction of acetophenone into phenylethanol. The combinatorial approach was based on evolution of a first library containing 60 ligands. For the evolution, operators such as replication, regression, cross-over and mutation were used. The study was performed with a XYZ robot and fast chiral GC analysis. Over only 4 generations, the average targeted criterion, enantioselectivity, was increased from 20% to ca. 80% for the 4th generation. The best results provided enantiomeric excess up to 93%.

Cite this article as:

Abdallah Radwan, Grenouillet Pierre, Vriamont Nicolas, Riant Olivier and de Bellefon Claude, High Throughput Screening and Evolution of a Library of Ligands in Asymmetric H-Transfer Reduction of Acetophenone, Combinatorial Chemistry & High Throughput Screening 2010; 13 (5) . https://dx.doi.org/10.2174/138620710791292985