Partially Saturated Bicyclic Heteroaromatics as an sp(3) -Enriched Fragment Collection.
Angew Chem Int Ed Engl
; 55(40): 12479-83, 2016 09 26.
Article
en En
| MEDLINE
| ID: mdl-27596095
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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01-internacional
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MEDLINE
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En
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Angew Chem Int Ed Engl
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2016
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Article