Cartwright, Matthew William (2006) Highly functionalised fused heterocycle synthesis from fluoropyridines. Doctoral thesis, Durham University.
|Archive (ZIP) (Crystal structures data tables) - Supplemental Material|
Current approaches to drug discovery tends to involve the rapid analogue synthesis and testing of small, focused libraries of low molecular weight, structurally similar "drug-like" molecules, often based around heterocyclic core scaffolds. If some desired activity is shown by a compound, elaboration can give higher activity and more favourable pharmiokinetic properties. As this "lead generation" stage of drug development has been identified as a major bottleneck in the drug pipeline process, there is a great demand for methodology detailing the synthesis of highly functionalised heterocyclic compounds. Our approach involves the sequential nucleophilic aromatic substitution of highly fluorinated pyridines, in an efficient and flexible manner, to furnish a range of novel, functionalised polycyclic systems.
|Item Type:||Thesis (Doctoral)|
|Award:||Doctor of Philosophy|
|Copyright:||Copyright of this thesis is held by the author|
|Deposited On:||09 Sep 2011 09:51|