Themodernbillion-dollardrug-discoveryprocessstronglyreliesonbothhi- throughput synthesis and screening methods. Whereas the latter is based on molecular biological methods, the ef?cient and reliable generation of c- pound collections often makes use of combinatorial chemistry. Discovered in the 1980s, this methodology was explored extensively in the 1990s by groups in academia and in industry. Without any doubt, combinatorial chemistry changed the whole drug-discovery process and found many applications in cropscience and the material sciences. However, since its implementation, solution- and...

Themodernbillion-dollardrug-discoveryprocessstronglyreliesonbothhi- throughput synthesis and screening methods. Whereas the latter is based on molecular biological methods, the ef?cient and reliable generation of c- pound collections often makes use of combinatorial chemistry. Discovered in the 1980s, this methodology was explored extensively in the 1990s by groups in academia and in industry. Without any doubt, combinatorial chemistry changed the whole drug-discovery process and found many applications in cropscience and the material sciences. However, since its implementation, solution- and...