Diversity-oriented synthesis

Diversity-oriented synthesis aims to produce chemical libraries that are representative of a large portion of chemical space by applying a variety of reaction conditions to starting materials with multiple different functional groups. Multiple rounds of such reactions result in rapid access to structurally diverse products suitable for screening.

Latest Research and Reviews

News and Comment

  • News & Views |

    Natural products often provide lead scaffolds for the development of therapeutics, but complexity of their synthesis can limit the discovery of improved analogues. Pharmacophore-directed retrosynthesis aims to accelerate the building of a structure–activity relationship profile of a natural product, aiming to identifying a simplified lead.

    • Jason R. Hudlicky
    •  & Gary A. Sulikowski
    Nature Chemistry 11, 297-298
  • News & Views |

    Natural products often serve as sources of new drugs, either directly or after synthetic modification, but site-selective functionalization of complex small molecules is challenging. Now, a method has been developed that enables selective modification of a wide range of natural products by engaging a benzyne intermediate in a variety of reaction modes.

    • Sarah Z. Tasker
    •  & Paul J. Hergenrother
    Nature Chemistry 9, 504-506
  • Comments & Opinion |

    Adam Nelson and Stuart Warriner, from the University of Leeds, talk with Nature Chemistry about their work to develop viable synthetic strategies for preparing new chemical structures in parallel with the identification of desirable biological activity.

    • Stephen Davey
    Nature Chemistry 6, 845-846
  • News & Views |

    Two approaches have emerged for creating libraries of compounds for use in biological screening assays for drug discovery — fragment-based ligand design and diversity-oriented synthesis. Advocates of each approach discuss their favoured strategy.

    • Philip J. Hajduk
    • , Warren R. J. D. Galloway
    •  & David R. Spring
    Nature 470, 42-43