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A Mild and Simple Method for Making MIDA Boronates

preprint
submitted on 31.03.2020, 17:47 and posted on 03.04.2020, 18:11 by Aidan Kelly, Peng-Jui (Ruby) Chen, Jenna Klubnick, Daniel J. Blair, Martin D. Burke

Existing methods for making MIDA boronates require harsh conditions and complex procedures to achieve dehydration. Here we disclose that a pre-dried form of MIDA, MIDA anhydride, acts as both a source of the MIDA ligand and an in situ desiccant to enable a mild and simple MIDA boronate synthesis procedure. This method expands the range of sensitive boronic acids that can be converted into their MIDA boronate counterparts. Further utilizing unique properties of MIDA boronates, we have developed a MIDA Boronate Maker Kit which enables the direct preparation and purification of MIDA boronates from boronic acids using only heating and centrifuge equipment that is widely available in labs that do not specialize in organic synthesis.

Funding

National Institutes of Health (GM118185)

Damon Runyon Cancer Research Foundation (DRG-2290–17)

History

Email Address of Submitting Author

danielb@illinois.edu

Institution

University of Illinois at Urbana-Champaign

Country

United States of America

ORCID For Submitting Author

0000-0002-2279-7538

Declaration of Conflict of Interest

The University of Illinois at Urbana Champaign (UIUC) has filed patent applications involving MIDA boronates which have been licensed to REVOLUTION Medicines, a company for which MDB is a Founder and Consultant.

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