Archived: Deuterium in Organic Chemistry and Drug Discovery
Date: 14 November 2018
Time: 15:00 - 16:00 GMT
This FREE to attend webinar was presented by Dr John Studley, Scientific Update.
John will cover the following topics:
- General introduction-, discovery, natural abundance etc
- Why is deuterium of interest to chemists?
- Physical properties and comparison to proteo- compounds
- Applications
- Key articles to read for further information
- D2 and D2O
- Methods of production in the lab and commercial production processes
- Girdler sulphide process
- Suppliers of deuterated raw materials intermediates and prices
- How are deuterated solvents made?
- Shipping deuterated raw materials
- Analysis of deuterated organic compounds
- Mass spec and NMR
- Isotopic purity
- Deuterium kinetic isotope effect (examples)
- Deuterium tracer for reaction mechanism elucidation
- Deuterium in drug discovery and development
- Stable isotope labels
- In vivo effects of deuterium containing compounds (PK/PD effects)
- Elucidation of metabolic pathways
- Deuterium in medicinal chemistry- “leaving the label in the drug”
- Deutetrabenazine- the first FDA approved (2017) deuterated drug (mechanism, benefit)
- Deuterated Linoleic acid and use of deuterium to reinforce oxidation-vulnerable C-H bonds within nutrients
- Examples of other deuterated compounds in development
- Big pharma pipelines
- Concert pharmaceuticals model
- Several case studies and examples
- Regulatory issues
- FDA 505 (b)(2) and 21 U.S.C. 355(b)(2)
- Expedited rote to approval
- Patent issues and obviousness analysis
- Methods for synthesising deuterium labelled compounds
- Deuterated reagents (e.g. LiAlD4, LiBD4, NR3.BD3)
- MacMillan’s photoredox approach to deuterated API’s
- C-H functionalization approaches
- Metal-mediated approaches
- Alpha-deuteration of amino acids and amines at scale
- Incorporation of deuterium into heterocycles
- Introduction to the use of Tritium
- Short introduction to other isotopes- C13, C14, N15 and radio-isotopes