Juan Zhang; Xianfeng Li; Haimei Wei; Yangfeng Li; Gong Zhang; Yizhou Li
Org. Lett., 2021, 23(21), 8429-8433
https://doi.org/10.1021/acs.orglett.1c03145

Abstract

The construction of chemical libraries containing polysubstituted pyrazoline scaffolds is highly desirable for the discovery of novel chemical ligands for biological targets. Herein, we report a sequential DNA-encoded synthesis strategy for polysubstituted pyrazoline heterocycles, which fuses a broad panel of aldehydes, aryl amines, and alkenes as building blocks. Furthermore, mock library synthesis and selection demonstrated the ability of the method to produce DNA-encoded focused libraries with highly functionalized pyrazoline cores.