Welcome to HitGen


Enable Innovative Drug Discover with DEL, FBDD and SBDD

  1. 关于我们
  2. Publications

On-DNA Decarboxylative Arylation: Merging Photoredox with Nickel Catalysis in Water 发布时间:2019-06-21


A new catalytic manifold that merges photoredox with nickel catalysis in aqueous solution is presented. Specifically, the combination of a highly active, yet air-stable, nickel precatalyst with a new electron-deficient pyridyl carboxamidine ligand was key to the development of a water-compatible nickel catalysis platform, which is a crucial requirement for the preparation of DNA-encoded libraries (DELs). Together with an iridium-based photocatalyst and a powerful light source, this dual catalysis approach enabled the efficient decarboxylative arylation of α-amino acids with DNA-tagged aryl halides. This C(sp2)–C(sp3) coupling tolerates a wide variety of functional groups on both the amino acid and the aryl halide substrates. Due to the mild and DNA-compatible reaction conditions, the presented transformation holds great potential for the construction of DELs. This was further evidenced by showing that well plate-compatible LED arrays can serve as competent light sources to facilitate parallel synthesis. Lastly, we demonstrate that this procedure can serve as a blueprint toward the adaptation of other established nickel metallaphotoredox transformations to the idiosyncratic requirements of a DEL.

ACS Comb. Sci. 2019, 21, 8, 588–597


Link: https://pubs.acs.org/doi/abs/10.1021/acscombsci.9b00076

Thanks for reading!

For more details on how we can advance your innovative drug discovery projects
By submitting your information, you acknowledge having received, read and understood our Privacy Notice as made available above.

We use cookies to provide a better web experience.
By using our site, you acknowledge our use of cookies and please read our Cookie Notice for More information