ABSTRACT

Lilly Research Laboratories, A Division o f Eli Lilly and Company, Chemical Process Research and Development Division, Indianapolis, IN 46285

Milton J. Zmijewski

Lilly Research Laboratories, A Division o f Eli Lilly and Company, Natural Products Discovery Development Research, Indianapolis, IN 46285

Key words: AMPA receptor antagonist; yeast; reduction; resin; isochroman; autoxidation

Introduction

Benzodiazepines serve a central role in drug therapies which target central nervous system

disorders. Structure activity relationship (SAR) studies involving these agents have inspired the

generation of thousands of analogs. The 1,4-benzodiazepine ring system, represented by clinically

important drugs such as Diazepam (Valium®), has been the principal focus of much of this work.1

Hungarian researchers at the Institute of Drug Research, however, have centered a drug discovery

program on the structurally and pharmacologically distinct class of 2,3-benzodiazepine