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High-yield and high-purity amide bond formation using DMTMM PF 6 for DNA-encoded libraries.

Authors :
Hosozawa T
Niwa M
Takeuchi H
Inohana T
Okumura K
Itoh S
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2024 Sep 15; Vol. 110, pp. 129859. Date of Electronic Publication: 2024 Jun 30.
Publication Year :
2024

Abstract

In this study, we report on the ability of DMTMM PF <subscript>6</subscript> to improve the amidation reaction. The on-DNA amidation reaction using DMTMM PF <subscript>6</subscript> demonstrates higher conversion rates than those using HATU or DMTMM Cl, particularly with challenging sterically hindered amines and carboxylic acids. The developed method enables the expansion of available building blocks and the efficient synthesis of high-purity DNA-encoded libraries.<br />Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br /> (Copyright © 2024 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
110
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
38955244
Full Text :
https://doi.org/10.1016/j.bmcl.2024.129859