Combinatorial chemistry Introduction

Szostak JW (1997) Introduction Combinatorial Chemistry. Chem. Rev. 97 347-348, and all papers in the same issue... 

As C-C bond formation is an important step in organic synthesis, particularly for pharmaceutical applications, it is useful to look for operation modes of chemical micro processing that allow one to carry out combinatorial chemistry investigations. As such, the serial introduction of multiple reactant streams by flow switching was identified [66,67]. The wide availability of precursors for acyiiminium cations has led to the expression cation pool [66, 67]. 

The number of candidate drugs has increased drastically since the introduction of combinatorial chemistry.13 One drawback is that the compounds generated often do not have favorable biopharma-ceutical and pharmacokinetic properties.1314 For example, drug candidates may be poorly soluble in water, leading to low drug concentrations in GI fluids.1314 Forty percent of late stage failures are linked to poor pharmacokinetic properties.15... 

Introduction Current Challenges in Combinatorial Chemistry Research... 

As mentioned earlier in the Introduction, combinatorial and parallel chemistry have emerged as novel technologies to provide libraries of diverse compounds. The basic idea of combinatorial chemistry is to synthesize starting e.g. from building blocks A, B, C1, C2, and C3 (Figures 11-13) all possible combinations of products (P -P3) as single compounds, or as mixtures on solid supports, or in solution. These compounds can be synthesized in a parallel or in a combinatorial fashion using the... 

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