Deuterium in Organic Chemistry and Drug Discovery

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