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Oxalyl boronates enable modular synthesis of bioactive imidazoles

Abstract:

Described herein is the preparation of oxalyl boronate building blocks and their application for the construction of heterocycles. The oxalyl unit, readily accessible through commercially available starting materials, enables a modular approach for the synthesis of imidazoles. A variety of aromatic, heteroaromatic, and alkyl carboxaldehydes were condensed with oxalyl boronates to afford substituted boryl imidazoles in a regiocontrolled fashion. Subsequent palladium-catalyzed cross-coupling wi...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Accepted Manuscript

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Publisher copy:
10.1002/anie.201611006

Authors


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Department:
Oxford, MSD, NDM, Target Discovery Institute
Role:
Author
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Department:
Oxford, MSD, NDM, Structural Genomics Consortium
Role:
Author
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Natural Sciences and Engineering Research Council of Canada More from this funder
Canadian Institute of Health Research More from this funder
Publisher:
Wiley-VCH Verlag Publisher's website
Journal:
Angewandte Chemie International Edition Journal website
Volume:
56
Issue:
22
Pages:
6264-6267
Publication date:
2017-03-07
DOI:
EISSN:
1521-3773
ISSN:
1433-7851
Pubs id:
pubs:685508
URN:
uri:859d7d70-a6a0-4a34-af71-44894cac8fd1
UUID:
uuid:859d7d70-a6a0-4a34-af71-44894cac8fd1
Local pid:
pubs:685508
Paper number:
22

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