4.6 Article

Palladium-Mediated Hydroamination of DNA-Conjugated Aryl Alkenes

Journal

FRONTIERS IN CHEMISTRY
Volume 10, Issue -, Pages -

Publisher

FRONTIERS MEDIA SA
DOI: 10.3389/fchem.2022.851674

Keywords

DNA-encoded library; palladium catalysis; C-N bond formation; DNA-conjugated aryl ethylene; hydroamination

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An efficient Pd-promoted hydroamination reaction for the formation of C(sp(3))-N bonds on DNA was reported. This transformation has significant potential for applications in medicinal chemistry and DNA-encoded library synthesis.
C-N bond formation is one of the most commonly used reactions in medicinal chemistry. Herein, we report an efficient Pd-promoted hydroamination reaction between DNA-conjugated aryl alkenes and a wide scope of aliphatic amines. The described reactions are demonstrated in good to excellent conversions to furnish C (sp(3))-N bonds on DNA. This DNA-compatible transformation has strong potentials for the application into DNA-encoded library synthesis.

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