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RASS‐Enabled S/P−C and S−N Bond Formation for DEL Synthesis
Author(s) -
Flood Dillon T.,
Zhang Xuejing,
Fu Xiang,
Zhao Zhenxiang,
Asai Shota,
Sanchez Brittany B.,
Sturgell Emily J.,
Vantourout Julien C.,
Richardson Paul,
Flanagan Mark E.,
Piotrowski David W.,
Kölmel Dominik K.,
Wan Jinqiao,
Tsai MeiHsuan,
Chen Jason S.,
Baran Phil S.,
Dawson Philip E.
Publication year - 2020
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201915493
Subject(s) - suite , reactivity (psychology) , chemistry , combinatorial chemistry , dna , aqueous solution , encoding (memory) , nanotechnology , computational biology , computer science , materials science , biology , organic chemistry , biochemistry , political science , medicine , artificial intelligence , alternative medicine , pathology , law
DNA encoded libraries (DEL) have shown promise as a valuable technology for democratizing the hit discovery process. Although DEL provides relatively inexpensive access to libraries of unprecedented size, their production has been hampered by the idiosyncratic needs of the encoding DNA tag relegating DEL compatible chemistry to dilute aqueous environments. Recently reversible adsorption to solid support (RASS) has been demonstrated as a promising method to expand DEL reactivity using standard organic synthesis protocols. Here we demonstrate a suite of on‐DNA chemistries to incorporate medicinally relevant and C−S, C−P and N−S linkages into DELs, which are underrepresented in the canonical methods.