期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 56, 期 22, 页码 6264-6267出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201611006
关键词
biological activity; boron; cross-coupling; heterocycles; synthetic methods
资金
- Natural Science and Engineering Research Council (NSERC)
- Canadian Institute of Health Research (CIHR)
- Astex Pharmaceuticals
- Canadian Foundation for Innovation [19119]
- Ontario Research Fund
- NSERC
- Government of Ontario
- OGS
- AbbVie [1097737]
- Bayer Pharma AG
- Boehringer Ingelheim
- Canada Foundation for Innovation
- Eshelman Institute for Innovation
- Genome Canada
- Innovative Medicines Initiative (EU/EFPIA) [ULTRA-DD] [115766]
- Janssen
- Merck Co.
- Novartis Pharma AG
- Ontario Ministry of Economic Development and Innovation
- Pfizer
- Sao Paolo Research Foundation-FAPESP
- Takeda
- Wellcome Trust [106169/ZZ14/Z]
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 with haloarenes furnished the desired trisubstituted imidazole scaffolds. To demonstrate the utility of these scaffolds, potent inhibitors of the serine/threonine-protein kinase STK10 were synthesized.
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