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Rapid Approach to Complex Boronic Acids

Rapid Approach to Complex Boronic Acids

Constantinos G Neochoritis, Shabnam Shaabani, Maryam Ahmadianmoghaddam, Tryfon Zarganes-Tzitzikas, Li Gao, Michaela Novotná, Tatiana Mitríková, Atilio Reyes Romero, Marina Ika Irianti, Ruixue Xu, Joe Olechno, etc.

Sci Adv. 2019 Jul 5;5(7):eaaw4607.

PMID: 31281893

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1287753427	(6-Methyl-5-quinolinyl)boronic acid		1287753-42-7	Price

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