Partially Saturated Bicyclic Heteroaromatics as an sp3‐Enriched Fragment Collection |
| |
| Authors: | David G. Twigg Dr. Noriyasu Kondo Sophie L. Mitchell Dr. Warren R. J. D. Galloway Dr. Hannah F. Sore Dr. Andrew Madin Prof. David R. Spring |
| |
| Affiliation: | 1. Department of Chemistry, University of Cambridge, Cambridge, UK;2. Shionogi & Co. Ltd., Osaka, Japan;3. AstraZeneca UK Ltd., Cambridge, UK |
| |
| 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 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. |
| |
| Keywords: | drug design drug discovery fused-ring systems nitrogen heterocycles synthetic methods |
|
|
