Combinatorial chemistry (1 –7 ) has drastically modified the drug discovery process by allowing the rapid simultaneous preparation of numerous organic molecules to feed bioassays. Most of the time, syntheses are carried out using solid-phase methodology (8 ). The target compounds are built on an insoluble support (resins, plastic pins, etc). Reactions are driven to completion by the use of excess reagents. Purification is performed by extensive washing of the support. Finally, the molecules are released in solution upon appropriate chemical treatments.