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  • Review Article
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Contemporary screening approaches to reaction discovery and development

Nature Chemistry volume 6, pages 859–871 (2014)Cite this article

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Abstract

New organic reactivity has often been discovered by happenstance. Several recent research efforts have attempted to leverage this to discover new reactions. In this Review, we attempt to unify reported approaches to reaction discovery on the basis of the practical and strategic principles applied. We concentrate on approaches to reaction discovery as opposed to reaction development, though conceptually groundbreaking approaches to identifying efficient catalyst systems are also considered. Finally, we provide a critical overview of the utility and application of the reported methods from the perspective of a synthetic chemist, and consider the future of high-throughput screening in reaction discovery.

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Figure 1: Representative chemistries developed using the first high-throughput screening and combinatorial approaches.
Figure 2: Novel reactivity discovered using multidimensional screens.
Figure 3: Sandwich immunoassays.
Figure 4: DNA-templated synthesis in reaction discovery.
Figure 5: Reactions discovered using matrix-assisted laser desorption/ionization-derived analysis techniques.
Figure 6: Exploiting colourimetry and fluorescence in reaction development.
Figure 7: Application of enzyme-based screening in reaction development.
Figure 8: Screening of reaction intermediates and transition states.

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Acknowledgements

We are grateful to the European Research Council (ERC) under the European Community's Seventh Framework Program (FP7 2007-2013)/ERC grant agreement no 25936, and the DFG (Leibniz award) for generous financial support.

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  1. Organisch-Chemisches Institut, Westfälische Wilhelms-Universität Münster, Corrensstrasse 40, Münster, 48149, Germany

    Karl D. Collins, Tobias Gensch & Frank Glorius

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  1. Karl D. Collins
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  2. Tobias Gensch
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  3. Frank Glorius
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Correspondence to Karl D. Collins or Frank Glorius.

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Collins, K., Gensch, T. & Glorius, F. Contemporary screening approaches to reaction discovery and development. Nature Chem 6, 859–871 (2014). https://doi.org/10.1038/nchem.2062

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