The second talk described below may be of interest
*JEOL Postdoc Competition Winners’ Seminar *
*Thursday 20th September *
*13.00-15.00*
*C/A101*
*13.00 Dr. Aggie Lawer*
*"Synthesis of functionalised peptides/macrocycles and medium-size **rings
via stereoselective fluorination and SuRE/NICE chemistry"*
Insertion of fluorine into organic molecules is well-known to affect the
molecules’ electronic distribution and conformation in ways that can be
beneficial in drug development. However, the effects of fluorination have
not been widely investigated in the context of peptides, which limits the
development of peptide-based drugs. In the first part of the talk, I will
discuss how stereoselective fluorination was used to control the conformations
of peptides and enhance the potency of a peptide-based enzyme inhibitor. While
peptides/macrocycles and medium-size rings have recently gained
noteworthy interest
in the area of medicinal chemistry, their synthesis is mostly limited to
the traditional end-to-end macrocyclisations which suffer from unfavourable
thermodynamic factors, and oftentimes require the use of high dilution
conditions. In the second part of my talk, I’ll describe how Successive
Ring Expansion (SuRE) and N-acyl Iminium ion mediated Cyclisation/Expansion
(NICE) reactions developed in Unsworth group could be employed to overcome
these limitations, providing an efficient, scalable and practical route to
make diverse macrocycles and medium-size rings.
*13.45 Dr. Peter Rayner *
*"Tunable Hyperpolarisation by Synthetic Design"*
NMR and MRI are two of the most popular techniques to study molecules and
materials. However, both of these approaches are insensitive and
hyperpolarization methods to increase signal size are needed in order to
access new applications. This talk will describe how rational synthetic
design of both the contrast agents and N-heterocyclic carbene catalysts
utilized in the Signal Amplification by Reversible Exchange process, have
led to signals that are up to 120,000 times larger than those achieved on a
typical hospital scanner and can be observed many minutes after their
creation. These improvements have allowed the observation of hyperpolarized
molecules by in vivo MRI techniques.
*The seminar will be followed at 14.30 by refreshments*
--
Antony Morland, PhD.
Director, York Neuroimaging Centre
Department of Psychology, University of York, York YO10 5DD, UK.
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