Synthetic library techniques: Subjective (biased and generic) thoughts and views

Abstract

Various aspects of synthetic diversity generation and screening are discussed. Controversial issues are raised and different points of view are presented. We hope the article will stimulate thinking about the utilization of library techniques and start a discussion about questions concerning their application.

The “One-Bead-One-Compound” Combinatorial Library Method

“…Currently, the major effort in combinatorial chemistry is focused on combinatorial libraries of nonpeptide-like small molecules, reviewed e.g. in refs , , , , , , and 145. The rational for this activity is 2-fold.…”

Parallel Personal Comments on “Classical” Papers in Combinatorial Chemistry

“…Back when we were discussing the question of “Who is the father of molecular diversity?” in the rather controversial review article written with Viktor Krchňák (one referee suggested that this type of article should never be published in a scientific journal, the second referee recommended the publication with high priority), we concluded that there is no “father of diversity”. However, there is a “Mother of diversity”Mother Nature.…”

An automated system for the purification of combinatorial libraries by preparative LC/MS

“…Hundreds of new drug candidates can be produced simultaneously by a single medicinal chemist with the aid of laboratory robotic equipment to automate solid-phase or solutionphase synthesis in parallel. Much of the research in combinatorial chemistry has focused on developing synthetic methodologies [3] and instrumentation [4] for generating libraries of compounds. There has been comparatively less attention paid to the development of automated systems designed to handle the purification requirements imposed by parallel synthesis.…”