Details

Autor(en) / Beteiligte

• Patel, Shivani
• Badir, Shorouk O.
• Molander, Gary A.

Titel

Developments in Photoredox-Mediated Alkylation for DNA-Encoded Libraries

Ist Teil von

• Trends in chemistry, 2021-03, Vol.3 (3), p.161-175

Ort / Verlag

United States: Elsevier Inc

Erscheinungsjahr

2021

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• Recently, DNA-encoded library (DEL) technology has emerged as an innovative screening modality for the rapid discovery of therapeutic candidates in pharmaceutical settings. This platform enables a cost-effective, time-efficient, and large-scale assembly and interrogation of billions of small organic ligands against a biological target in a single experiment. An outstanding challenge in DEL synthesis is the necessity for water-compatible transformations under ambient conditions. To access uncharted chemical space, the adoption of photoredox catalysis in DELs, including Ni-catalyzed manifolds and radical/polar crossover reactions, has enabled the construction of novel structural scaffolds through regulated odd-electron intermediates. Herein, a critical discussion of the validation of photoredox-mediated alkylation in DEL environments is presented. Current synthetic gaps are highlighted and opportunities for further development are speculated upon. DNA-encoded library (DEL) technology has emerged as an innovative screening modality for exploration of uncharted chemical space in the pharmaceutical industry.Through single-electron-transfer (SET), odd-electron intermediates are generated in a regulated fashion under mild reaction conditions.Photoredox-mediated alkylation allows rapid assembly of molecular complexity in DELs while retaining high functional group tolerance.