ArticleAdvanced science (Weinheim, Baden-Wurttemberg, Germany)2024
Mask and Release Strategy-Enabled Diversity-Oriented Synthesis for DNA-Encoded Library.
Article in Advanced science (Weinheim, Baden-Wurttemberg, Germany), 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed.
- Highly selective and AI-predictable Se-N exchange chemistry between benzoselenazolones and boronic acids for programmable, parallel, and DNA-encoded library synthesis.Chemical science · 2026Article
- Synthesis of 3,3-oxaspirocycles via cobalt-catalyzed cascade C-H activation and carboamidation of alkynes.Communications chemistry · 2025Article
- Translation of Deoxyribonucleic Acid into Synthetic Alpha Helical Peptides for Darwinian Evolution.JACS Au · 2024Article
- FSOACS medicinal chemistry letters · 2024Article
- Mask and Release Strategy-Enabled Diversity-Oriented Synthesis for DNA-Encoded Library.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
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Authors and funding
10 authors.
Funding
Abstract
An ideal DNA-encoded library (DEL) selection requires the library to consist of diverse core skeletons and cover chemical space as much as possible. However, the lack of efficient on-DNA synthetic approaches toward core skeletons has greatly restricted the diversity of DEL. To mitigate this issue, this work disclosed a "Mask & Release" strategy to streamline the challenging on-DNA core skeleton synthesis. N-phenoxyacetamide is used as a masked phenol and versatile directing group to mediate diversified DNA-compatible C-H functionalization, introducing the 1st-dimensional diversity at a defined site, and simultaneously releasing the phenol functionality, which can facilitate the introduction of the 2nd diversity. This work not only provides a set of efficient syntheses toward DNA-conjugated drug-like core skeletons such as ortho-alkenyl/sulfiliminyl/cyclopropyl phenol, benzofuran, dihydrobenzofuran but also provides a paradigm for on-DNA core skeleton synthetic method development.
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Registered trials
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