On-DNA Alkyne Iodination and Acetylenic Coupling as a Useful Tool for DEL Synthesis

Ayun Luo; Hongxia Zhou; Qi Zhou; Qini Hua; Xue Zhao; Xiaobing Yu; Kexin Yang; Yunjin Hu
Bioconjugate Chem., 2022, 33(12), 2299-2306
https://doi.org/10.1021/acs.bioconjchem.2c00471

Abstract

1-Iodoalkynes and 1,3-diynes are versatile chemical intermediates and pharmaceutically valuable ingredients. In this study, copper mediated on-DNA alkyne iodination and Cadiot-Chodkiewicz coupling are developed for the first time. This generates diverse, systematic, and unprecedented topographic structural features, which could be invaluable as molecular recognition agents for drug discovery in DEL screening.

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