Contemporary screening approaches to reaction discovery and development

Nat Chem. 2014 Oct;6(10):859-71. doi: 10.1038/nchem.2062.


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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Catalysis
  • Combinatorial Chemistry Techniques
  • Cycloaddition Reaction
  • DNA / chemistry
  • DNA / metabolism
  • High-Throughput Screening Assays
  • Immunoassay
  • Organic Chemicals / chemical synthesis
  • Organic Chemicals / chemistry
  • Pharmaceutical Preparations / chemical synthesis*
  • Pharmaceutical Preparations / chemistry
  • Solid-Phase Synthesis Techniques
  • Substrate Specificity


  • Organic Chemicals
  • Pharmaceutical Preparations
  • DNA