Ruthenium-Mediated [2 + 2 + 2] Cyclization: A Route to Forge Indane and Isoindoline Core and Its Application in DNA-Encoded Library Technology

Autor:	Yanrui Suo, Min Xu, Meimei Sun, Weiwei Lu, Xuan Wang, Xiaojie Lu
Rok vydání:	2022
Předmět:	Technology Cyclization Organic Chemistry DNA Physical and Theoretical Chemistry Biochemistry Ruthenium
Zdroj:	Organic Letters. 24:9092-9096
ISSN:	1523-7052 1523-7060
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::28e85d2318e46eae2b4609dc6664ff20 https://doi.org/10.1021/acs.orglett.2c03759 Zobrazit plný text záznamu