On-DNA Mannich Reaction for DNA-Encoded Library Synthesis.

Autor: Ryzhikh D; KNU G-LAMP Project Group, KNU Institute of Basic Sciences, Department of Chemistry, Kyungpook National University, Daegu 41566, Republic of Korea., Seo H; New Drug Development Center (NDDC), Daegu-Gyeongbuk Medical Innovation Foundation (K-MEDI hub), Daegu 41061, Republic of Korea., Lee J; New Drug Development Center (NDDC), Daegu-Gyeongbuk Medical Innovation Foundation (K-MEDI hub), Daegu 41061, Republic of Korea., Lee J; New Drug Development Center (NDDC), Daegu-Gyeongbuk Medical Innovation Foundation (K-MEDI hub), Daegu 41061, Republic of Korea., Nam MH; Metropolitan Seoul Center, Korea Basic Science Institute (KBSI), Seoul 02841, Republic of Korea., Song M; New Drug Development Center (NDDC), Daegu-Gyeongbuk Medical Innovation Foundation (K-MEDI hub), Daegu 41061, Republic of Korea., Hwang GT; KNU G-LAMP Project Group, KNU Institute of Basic Sciences, Department of Chemistry, Kyungpook National University, Daegu 41566, Republic of Korea.
Jazyk: angličtina
Zdroj: The Journal of organic chemistry [J Org Chem] 2024 Nov 15; Vol. 89 (22), pp. 16957-16963. Date of Electronic Publication: 2024 Nov 01.
DOI: 10.1021/acs.joc.4c02098
Abstrakt: 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.
Databáze: MEDLINE