Copper-Mediated Three-Component Reaction for the Synthesis of N‑Acylsulfonamide on DNA

The DNA-encoded library (DEL) technology is a new method for discovering hit compounds for target proteins in the pharmaceutical industry. The N-acylsulfonamide functional group has been reported to exhibit various pharmacological activities, and based on this, the demand for a method that allows it...

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Bibliographic Details
Published in:Organic letters 2022-07, Vol.24 (27), p.4881-4885
Main Authors: Eom, Solji, Kwon, Taeyeon, Lee, Da Yeon, Park, Chi Hoon, Kim, Hyun Jin
Format: Article
Language:English
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Summary:The DNA-encoded library (DEL) technology is a new method for discovering hit compounds for target proteins in the pharmaceutical industry. The N-acylsulfonamide functional group has been reported to exhibit various pharmacological activities, and based on this, the demand for a method that allows its introduction into the DEL platform has increased. In this report, a procedure for synthesizing N-acylsulfonamide functional groups applicable to DEL construction was developed in the presence of a copper reagent and water as a nucleophile from simple alkynes or sulfonyl azides, which are widely commercially available. Furthermore, we prove that a new alternative procedure can be used to construct a DNA-encoded library.
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.2c01675