Yanrui Suo; Min Xu; Meimei Sun; Weiwei Lu; Xuan Wang; Xiaojie Lu
Org. Lett., 2022, 24(49), 9092-9096
https://doi.org/10.1021/acs.orglett.2c03759

Abstract

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.