Zhaobing Ding; Yizhou Wu; Feifei Li; Siyu Jia; Bing Qi; Zuozhong Peng
Bioconjugate Chem., 2023, 34(9), 1523-1527
https://doi.org/10.1021/acs.bioconjchem.3c00291

Abstract

Here, we report a DNA-compatible reaction for the generation of cyclopropane derivatives using thiolides with α,β-unsaturated ketones in the absence of transition metal and N2 protection, which is convenient for DNA encoded library (DEL) construction. This approach allows the rapid and efficient production of a series of DEL libraries of potentially biologically active cyclopropanes and spirocyclopropyl oxindole derivatives.