General Remarks

Economic pressure to speed up the drug discovery process has had a huge impact on all fields of medicinal chemistry [1], therefore automation has increasingly become one of the main strategies to fulfill this demand [2]. While automation was successful in high-throughput screening (HTS) [3] and peptide synthesis, it played a minor role in mainstream organic synthesis. Automated systems are recommended for procedures that are highly predictable and repetitive [4]. However, organic chemistry is seldom defined in this way. The successful synthesis of organic molecules depends strongly on the chemical properties of the reagents and react-ants. Within the library production process solubility and reactivity of synthons can be highly different, therefore it is very difficult to find one protocol that works for every building block. Since multiple parallel synthesis began, there has been a wide range of different approaches and concepts for the design of automated systems to overcome these problems [5-7]. The first attempts at automation were the simple parallelization of commercially available reaction vessels. Secondly, reaction blocks were designed and used in combination with existing liquid-handling systems. Another approach uses stand alone systems that mimic the typical action of a chemist. Today, modern automated systems are modular workstation approaches. An overview is given in Table 6.1.

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