5 years ago

Ruthenium Promoted On-DNA Ring-Closing Metathesis and Cross-Metathesis

Ruthenium Promoted On-DNA Ring-Closing Metathesis and Cross-Metathesis
Christopher P. Davie, Christopher B. Phelps, Xiaojie Lu, Christine P. Donahue, Lijun Fan
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.

Publisher URL: http://dx.doi.org/10.1021/acs.bioconjchem.7b00292

DOI: 10.1021/acs.bioconjchem.7b00292

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