On September 2nd, 2022, Professor Li Yizhou group at the School of Pharmaceutical Science of Chongqing University published an article on Organic Letters entitled "On-DNA Synthesis of Functionalized 4H-Pyran Scaffolds for Focused DNA-Encoded Chemical Libraries".
As an important family of oxygen-containing heterocycles, functionalized 4H-pyran scaffolds can be widely found in many compounds with pharmacological properties ranging from antitumor and antimicrobial properties to calcium channel blocking properties. We here disclose its incorporation into DNA-encoded chemical libraries, combining this scaffold with the merits of scaffold architecture in drug design. Under the optimized DNA-compatible conditions, functionalized 4H-pyrans were efficiently formed with a broad substrate scope. Among the 4H-pyrans formed, the axial structure features rotational restriction, and the spirocyclic structure provides rigidity and three-dimensionality. These efforts open the door for the construction of DNA-encoded chemical libraries with more consideration for this structural architecture.
The first author of this article is Gao Yuting, a graduate student of Chongqing University. Li Yizhou, Li Yangfeng Zhang Gong are corresponding authors of this article.
Related link: https://pubs.acs.org/doi/10.1021/acs.orglett.2c02714
