Multifunctional Building Blocks Compatible with Photoredox-Mediated Alkylation for DNA-Encoded Library Synthesis.
Shorouk O. Badir,Jaehoon Sim,Katelyn Billings,Adam Csakai,Xuange Zhang,Weizhe Dong,Gary A. Molander +6 more
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TLDR
A photoredox-mediated cross-coupling and defluorinative alkylation process is introduced using commercially available alkyl bromides and structurally diverse α-silylamines for the incorporation of a variety of amino-acid-based organosilanes.About:
This article is published in Organic Letters.The article was published on 2020-01-15 and is currently open access. It has received 52 citations till now.read more
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Visible light photocatalysis in the late-stage functionalization of pharmaceutically relevant compounds.
Rolando Cannalire,Sveva Pelliccia,Luca Sancineto,Ettore Novellino,Gian Cesare Tron,Mariateresa Giustiniano +5 more
TL;DR: In this paper, the authors present a review of the recent developments in the field of late stage functionalization of complex biorelevant compounds and highlight the expected future progress and potential applications.
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Developments in Photoredox/Nickel Dual-Catalyzed 1,2-Difunctionalizations.
TL;DR: Recent advances in Ni/photoredox dual catalysis are explored, the current challenges are state, and perspectives on the design of new catalytic systems are discussed.
Journal ArticleDOI
Photocatalysis in the Life Science Industry.
Lisa Candish,Karl D. Collins,Gemma C. Cook,James Douglas,Adrián Gómez-Suárez,Anais Jolit,Sebastian Keess +6 more
TL;DR: In the pursuit of new pharmaceuticals and agrochemicals, chemists in the life science industry require access to mild and robust synthetic methodologies to systematically modify chemical structures, explore novel chemical space, and enable efficient synthesis.
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DNA-Encoded Chemistry: Drug Discovery from a Few Good Reactions
TL;DR: This review highlights the similarities between click and DEL reaction design and deployment in combinatorial library settings, providing a framework for the design of new DEL synthesis technologies to enable next-generation drug discovery.
Journal ArticleDOI
Encoded Library Technologies as Integrated Lead Finding Platforms for Drug Discovery.
TL;DR: This review discusses how encoded peptide libraries and DNA-encoded libraries are applied in research, and why Novartis considers it beneficial to run both pipelines in-house.
References
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Target-oriented and diversity-oriented organic synthesis in drug discovery.
TL;DR: Several synthetic planning principles for diversity-oriented synthesis and their role in the drug discovery process are presented in this review.
Journal ArticleDOI
The merger of transition metal and photocatalysis
TL;DR: The combination of Photoredox catalysis and transition metal catalysis is reviewed to show how this provides access to highly reactive oxidation states of transition metals and distinct activation modes that further enable the synthetic chemist.
Journal ArticleDOI
Analysis of Past and Present Synthetic Methodologies on Medicinal Chemistry: Where Have All the New Reactions Gone?
Dean G. Brown,Jonas Boström +1 more
TL;DR: It is shown that current practices result in overpopulation of certain types of molecular shapes to the exclusion of others using simple PMI plots, which could help catalyze improvements in integration of new synthetic methodologies as well as new library design.
Journal ArticleDOI
Encoded combinatorial chemistry.
Sydney Brenner,Richard A. Lerner +1 more
TL;DR: The diversity of chemical synthesis and the power of genetics are linked to provide a powerful, versatile method for drug screening that can be amplified by replication and utilized for enrichment of the bound molecules by serial hybridization to a subset of the library.
Journal ArticleDOI
Single-electron transmetalation in organoboron cross-coupling by photoredox/nickel dual catalysis
TL;DR: A mechanistically distinct single-electron transfer-based strategy for the activation of organoboron reagents toward transmetalation that exhibits complementary reactivity patterns.
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