Automated Organic Synthesis

A series of papers by Martin D. Burke and colleagues culminating in their most recent report (Li et al. Science 347, 1221-1226, 2015) describing automated synthesis of complex compounds from natural origins is impressive and the synthesis technology is expected to make a strong impact on pharmaceutical R&D.

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There is no doubt that automated organic synthesis schemes capable of efficiently producing large amounts of complex biologically relevant or drug-like compounds will spark the interest of many medicinal chemists and drug discovery researchers. The MIDA boronate-based coupling and purification technology introduced by Burke and co-workers to combine chemical building blocks into defined organic compounds is great in its simplicity and apparent robustness. Their prototypic three-module synthesizer can probably be further developed into a highly efficient machine for many synthetic pathways. Purists might argue, for example, that the art of organic synthesis is transformed into simplistic linear iterations or that the synthetic bandwidth of the technology is confined to pre-existing building blocks that encode desired chemistry, but this is not a major point, at least in my view. The arsenal of suitable building blocks can be further expanded and one certainly would not expect that all biologically relevant compound classes would soon be covered by this technology. Sure, similar to other automated approaches relevant for drug discovery R&D, non-experts might ultimately find (too) easy access to automated synthesis without a sound scientific foundation, which is not without problems, but the practical application potential of this technology can hardly be disregarded (and at its core is beautiful science, too). Today we take automated DNA or peptide synthesis for granted, and students are often unaware of the huge impact these technologies have made on the day-to-day life in research. So, any attempt to put synthetic efficiency onto a new level should be very interesting to follow, even for non-practitioners.

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Jürgen Bajorath

Professor , University of Bonn

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