Ruthenium-Mediated [2 + 2 + 2] Cyclization: A Route to Forge Indane and Isoindoline Core and Its Application in DNA-Encoded Library Technology
- Resource Type
- Authors
- Yanrui Suo; Min Xu; Meimei Sun; Weiwei Lu; Xuan Wang; Xiaojie Lu
- Source
- Organic Letters. 24:9092-9096
- Subject
- Technology
Cyclization
Organic Chemistry
DNA
Physical and Theoretical Chemistry
Biochemistry
Ruthenium
- Language
- ISSN
- 1523-7052
1523-7060
Indane and isoindoline are attractive bicyclic systems in biologically active compounds but are rarely reported in DNA-encoded libraries. In this paper, we reported an efficient and versatile approach for assembling indane and isoindoline scaffolds via a ruthenium-catalyzed [2 + 2 + 2] cyclotrimerization reaction. This method exhibits a broad substrate scope and has been successfully applied to construct a 53K-membered DNA-encoded library (DEL). In order to test its application, we carried out a preliminary selection of this DEL against Aurora A protein and identified a hit compound with 9.3 μM inhibition activity.