Development of a Micellar-Promoted Heck Reaction for the Synthesis of DNA-Encoded Libraries.

ABSTRACT: The capability of DNA encoded libraries (DELs) as a method of small molecule hit identification is becoming widely established in drug discovery. While their selection method offers advantages over more traditional means, DELs are limited by the chemistry that can be utilized to construct them. Significant advances in DNA compatible chemistry have been made over the past five years; however such procedures are still often burdened by substrate specificity and/or incomplete conversions, reducing the fidelity of the resulting libraries. One such reaction is the Heck coupling, for which current DNA-compatible protocols are somewhat unreliable. Utilizing micellar technology, we have developed a highly efficient DNA-compatible Heck reaction that proceeds on average to 95% conversion to product

SUBMITTER: Stanway-Gordon HA 

PROVIDER: S-EPMC10119937 | biostudies-literature | 2023 Mar

REPOSITORIES: biostudies-literature