Enzymatic Production of Chiral Pharmaceutical Building Blocks

Pharmaceuticals must typically be produced in the correct chiral form (enantiomer) to ensure high activity and avoid side effects. This process may require difficult chemical reactions, time and resource intensive separations, or expensive enantiomerically enriched starting materials. Properly chosen and tuned enzymatic reactions offer value because they specifically and efficiently produce desired enantiomers.

The market for pharmaceutical intermediates was worth $6.7 billion in 2006. The enzymes used to make many of these intermediates generated revenues of $198.0 million in 2006, and this market is expected to reach $354.4 million by 2013, driven largely by increased demand for chiral drug formulations (Source).

Dr. David Berkowitz and colleagues at the University of Nebraska Lincoln have developed novel enzymatic schemes to produce value-added chiral compounds with desired stereochemistry from inexpensive achiral starting materials. These products can be used as building blocks for a broad range of pharmaceuticals.

• Highly efficient and enantioselective method to produce value-added chiral building blocks from inexpensive achiral precursors
• Environmentally friendly process avoids heavy metal catalysts and organic solvents
• Generates intermediates that fit into known pathways for pharmaceutical manufacture
• Costly nicotinamide cofactors can be recycled using inexpensive reductants (3.4 –87¢/mol) obtained from discarded cellulosic biomass