DNA-Encoded Library Chemistry: Amplification of Chemical Reaction Diversity for the Exploration of Chemical Space

Ying Huang; Olena Savych; Yuii Moroz; Yiyun Chen; Robert A. Goodnow
Aldrichimica Acta, 2019, 52, 3, 75
https://www.sigmaaldrich.com/content/dam/sigma-aldrich/docs/Sigma-Aldrich/General_Information/2/acta-52-3-mk.pdf#page=63

Abstract

The use of DNA for encoding and decoding in smallmolecule synthesis for lead identification continues to gain widespread attention and application—more than a quarter century after its first disclosure. Successful execution of a diverse, drug-like library usually requires hundreds to thousands of commonly functionalized building blocks of relatively similar reactivity profiles. Aqueous and DNA-compatible organic reactions that utilize a large number of functionalized building blocks are perhaps among the most obvious and often discussed aspects of the successful application of this chemistry. This review highlights recent (since ~2015), relevant, new, and potentially highly useful such chemical transformations. Thereafter follows a discussion of the properties, requirements, costs, and diversity of building blocks that are currently available and may be useful for the construction of DNA-encoded libraries.

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