Combinatorial chemistry has significantly increased the speed of small molecule lead discovery and optimization for multiple targets in the pharmaceutical industry. Large libraries of bioactive compounds, synthesized either as mixtures or discreet units, can now be made using solid- or solution-phase techniques (1 -4 ). The design of the libraries can be biased toward a specific lead structure, enabling the rapid dissemination of information about the compound of interest (5 ,6 ). This chapter describes the methods developed for the application of combinatorial chemistry to the solid-phase synthesis of steroid receptor ligands.
