期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 55, 期 40, 页码 12479-12483出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201606496
关键词
drug design; drug discovery; fused-ring systems; nitrogen heterocycles; synthetic methods
资金
- EPSRC
- BBSRC
- MRC
- Wellcome Trust
- ERC [279337/DOS]
- AstraZeneca
- BASF
- Royal Society
- Engineering and Physical Sciences Research Council [EP/J016012/1, 1502976, EP/K039520/1, 1525290] Funding Source: researchfish
- EPSRC [EP/K039520/1, EP/J016012/1] Funding Source: UKRI
- European Research Council (ERC) [279337] Funding Source: European Research Council (ERC)
Fragment-based lead generation has proven to be an effective means of identifying high-quality lead compounds for drug discovery programs. However, the fragment screening sets often used are principally comprised of sp(2)-rich aromatic compounds, which limits the structural (and hence biological) diversity of the library. Herein, we describe strategies for the synthesis of a series of partially saturated bicyclic heteroaromatic scaffolds with enhanced sp(3) character. Subsequent derivatization led to a fragment collection featuring regio- and stereo-controlled introduction of substituents on the saturated ring system, often with formation of new stereocenters.
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