Partially Saturated Bicyclic Heteroaromatics as an sp³‐Enriched Fragment Collection

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 sp 2

Metal complexes for therapeutic applications

“…Despite the advantages of highly 3D molecules, modern drug discovery relies heavily on 2D and planar structures for both fragment and lead-like molecules [30,32,35]. Although there have been many recent efforts to design libraries comprising highly 3D molecules for drug discovery purposes [28,33,[36][37][38], most drug-like molecules trend toward planarity [32].…”

Emergent synthetic methods for the modular advancement of sp3-rich fragments

“…amide bond formations; reductive aminations). 26–29 However, in the absence of functionalisable synthetic handles, concerns may arise about the direct synthetic developability of sp 3 -rich fragments due to a lack of predictable synthetic methods to aid their advancement. 30 Indeed, pre-emptive development and exemplification of synthetic chemistries for direct fragment elaboration has recently been framed as a pressing challenge for the synthetic chemistry community.…”