| Autor: |
Twigg, DG, Kondo, N, Mitchell, SL, Galloway, WRJD, Sore, HF, Madin, A, Spring, DR |
| Přispěvatelé: |
Sore, Hannah [0000-0002-6542-0394], Spring, David [0000-0001-7355-2824], Apollo - University of Cambridge Repository |
| Jazyk: |
angličtina |
| Rok vydání: |
2016 |
| Předmět: |
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| Popis: |
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 sp²-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 sp³ 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. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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