Application of a Practical Biocatalytic Reduction to an Enantioselective Synthesis of the 5H-2,3-Benzodiazepine LY300164

Workers at the Hungarian Institute of Drug Research have recently discovered a novel class of orally active 2,3-benzodiazepines which serve as noncompetitive antagonists of the AMPA subtype of excitatory amino acid receptors. Preclinical studies have demonstrated that these compounds effectively block electroshock and chemically induced seizures in mice as well as provide neuroprotection from ischemic brain damage. One compound of particular interest in this class is the 5H-N-acetyl derivative, the more active species of which is the (-) isomer LY300164.