On-DNA Mannich Reaction for DNA-Encoded Library Synthesis

Danila Ryzhikh; Hyewon Seo; Jihoon Lee; Jieon Lee; Myung Hee Nam; Minsoo Song; Gil Tae Hwang
J. Org. Chem., 2024, 89(22), 16957–16963
https://doi.org/10.1021/acs.joc.4c02098

Abstract

The β-amino ketones produced through the Mannich reaction hold significant potential as candidates for various drugs. In this study, we optimized on-DNA Mannich reaction conditions and applied them to investigate the reactions of DNA-conjugated aldehydes with various amine and ketone building blocks. The developed on-DNA Mannich reaction preserved the DNA integrity and established viable routes for library production. These results underscore the potential of the Mannich reaction in DNA-encoded library (DEL) synthesis.

logo
logo