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Updated: Mar 1, 2026

Heterogeneous Removal of Water-Soluble Ruthenium Olefin Metathesis Catalyst from Aqueous Media Via Host-Guest Interaction
Published on: August 23, 2018
Ruthenium Promoted On-DNA Ring-Closing Metathesis and Cross-Metathesis
Xiaojie Lu1, Lijun Fan1, Christopher B Phelps1
1GlaxoSmithKline, Platform Technology & Science, Drug Discovery and Selection, New Chemical Entity Molecular Discovery, Encoded Library Technologies , 830 Winter Street, Waltham, Massachusetts 02451, United States.
Abstract:
DNA-encoded library technology (ELT) is now widely used in pharmaceutical, biotechnological, and academic research for hit identification and target validation. New on-DNA reactions are keys to exploring greater chemical space and accessing challenging chemotypes such as configurationally constrained macrocycles. Herein, we describe the first on-DNA ring-closing metathesis (RCM) and cross-metathesis (CM) reactions promoted by fast initiating Grubbs Ru reagents. Under the optimized conditions, MgCl2 was used to protect the DNA from Ru-induced decomposition. The substrate scope for on-DNA RCM was established and the same conditions were applied to a CM reaction with good conversion.
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