Partially Saturated Bicyclic Heteroaromatics as an spĀ³-Enriched Fragment Collection.
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Peer-reviewed
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Abstract
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 spĀ²-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 spĀ³ 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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Keywords
drug design, drug discovery, fused-ring systems, nitrogen heterocycles, synthetic methods
Journal Title
Angewandte Chemie International Edition
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Journal ISSN
1433-7851
1521-3773
1521-3773
Volume Title
55
Publisher
Wiley
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Sponsorship
European Research Council (279337)
Royal Society (WM150022)
Engineering and Physical Sciences Research Council (EP/J016012/1)
Engineering and Physical Sciences Research Council (EP/K039520/1)
Royal Society (WM150022)
Engineering and Physical Sciences Research Council (EP/J016012/1)
Engineering and Physical Sciences Research Council (EP/K039520/1)
EPSRC
BBSRC
MRC
Wellcome Trust
D.G.T. thanks AstraZeneca for funding. S.L.M. thanks BASF for funding. .