Actelion's Chemistry Group consists of highly experienced employees. They all benefit from sophisticated synthesis tools, analytical devices and automated purification systems.  Actelion's success in lead optimization is not only based on an efficient, project-oriented collaboration between medicinal chemists and parallel synthesis experts but also on a lively exchange between chemists and experts in pharmacology, structural biology and molecular modeling.

Automated Chemistry 

The major objective of the automated chemistry group is to deliver small focused libraries of purified compounds for lead optimization. This implies that the methodology used is restricted to solution-phase chemistry, which allows the synthesis of some hundred compounds per library.

The purification of all compounds represents the bottleneck in the whole process of synthesis, purification and analytics, but there are some significant advantages to be gained. For example, purification reduces the rate of decomposition of stored compounds, and the quality and comparability of all chemical and biological data are improved.

Synthesis

The equipment Actelion uses for the synthesis of small focused libraries are as varied as the chemistry, which has to be handled in a parallel approach.  The available tools range from a simple 96-deep-well plate in combination with a multichannel pipette, to completely automated liquid-handling systems.

Purification

One of the most important but time-consuming stages of every synthesis is the purification of products. To handle this bottleneck we use automated preparative HPLC systems that are able to purify up to 80 mixtures per day at a scale of 100 - 500 mg.

Analytics

For the rapid analysis of compounds and reaction mixtures, Actelion uses an automated HPLC-MPSS system. The use of an autosampler in combination with short run-times allows the analysis of up to 720 samples per day.