On-DNA Pd and Cu-Promoted C-N Cross-Coupling Reactions

Lu, X.; Wang, X.

Methods in Molecular Biology 2541: 49-54

2022


ISSN/ISBN: 1940-6029
PMID: 36083543
DOI: 10.1007/978-1-0716-2545-3_8
Accession: 080488460

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Summary
DNA-encoded library (DEL) recently has witnessed the swift development which has led to the new chemical entities identified for a wealthy biological interesting target; several small molecular inhibitors have moved into the late-stage clinical development. The success of DEL is heavily dependent on the chemical space which was assembled by the on-DNA chemical reactions. On-DNA C-N cross-coupling has great value for expanding the chemical space of DEL as amines are most abundant organic reagents available. Here we described the first on-DNA C-N cross-coupling reactions promoted by both Pd and Cu.