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The compatibility of free boronic acid building blocks in multicomponent reactions to readily create large libraries of diverse and complex small molecules was investigated. Traditionally, boronic acid synthesis is sequential, synthetically demanding, and time-consuming, which leads to high target synthesis times and low coverage of the boronic acid chemical space. We have performed the synthesis of large libraries of boronic acid derivatives based on multiple chemistries and building blocks using acoustic dispensing technology. The synthesis was performed on a nanomole scale with high synthesis success rates. The discovery of a protease inhibitor underscores the usefulness of the approach. Our acoustic dispensing-enabled chemistry paves the way to highly accelerated synthesis and miniaturized reaction scouting, allowing access to unprecedented boronic acid libraries.

Original publication

DOI

10.1126/sciadv.aaw4607

Type

Journal article

Journal

Science advances

Publication Date

07/2019

Volume

5

Addresses

Pharmacy Department, Drug Design group, University of Groningen, Deusinglaan 1, 9700 AV Groningen, Netherlands.

Keywords

Boronic Acids, Cyanides, Molecular Structure, Microwaves, Mass Spectrometry, Small Molecule Libraries