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Synthetic chemistry

ANSTO LifeSciences' synthetic chemistry capabilites and facilities are dedicated to research and development in organic chemistry, with a primary focus on organic compounds for radiochemistry applications.

The synthetic chemistry area is intrinsically linked with radiochemistry research and development in the design, synthesis and refinement of compounds for investigation, diagnosis and treatment of disease. Our staff are mainly PhD chemists with significant post-doctoral and industrial synthetic experience in the research and development of ligands to target disease. We operate in brand new, state-of-the-art laboratories, which are equipped with 14 fume cupboards, Nuclear Magnetic Resonance (NMR), Liquid Chromatography Mass Spectrometry(LCMS), High Performance Liquid Chromatography (HPLC) / automated flash chromatography (Grace Reveleris), peptide synthesiser, CEM microwave reactor, and MBraun solvent purifier. All facilities operate in compliance with current safety and environmental regulations. Complex products are produced in high purity, with a full quality control (?QC) analysis, suitable for in vivo analysis following radiolabelling and purification by our radiochemists.

Capabilities

Synthetic Organic Chemistry

  • Lab-scale synthesis of:
    • Organic compounds as precursors and standards for use in radiochemistry, especially 18F, 11C, 123I, 125I
    • Small compound libraries for structure-activity relationships, lead generation and optimisation
  • Halogenation chemistry
    • Incorporation of halogens onto compounds with known pharmacological properties
    • Radiohalogenation and in vivo evaluation (small animal, PET, SPECT)
  • Peptide synthesis
    • We utilise a Symphony Peptide Synthesiser in the synthesis of peptides, predominantly for radiochemistry applications
  • Custom synthesis
    • We custom synthesise radiolabelling precursors and standards for external collaborators
  • Synthetic capabilities
    • Acylation, alkylation, nucleophilic substitution, hydrogenation, oxidation, reduction, esterification, ether / amide synthesis, halogenation, synthesis of heterocycles, organometallic reactions, carbon-carbon bond formation,

IP Generation/Confidentiality

  • Development of Intellectual Property (IP) through novel applications of chemistry and radiochemistry is one of our primary goals, especially through the radiochemical derivatisation of compounds with known biological properties
  • Customers and collaborators can be completely assured of our confidentiality regarding proprietary technologies

Inorganic/Macrocyclic Chemistry

  • Incorporation of (radio)metals in macrocycles, development of metal chelates for radiometals

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Facilities

  • Bruker Spectrospin 400 MHz Ultrashield NMR Spectrometer
  • Waters Micromass ZQ Mass Spectrometer
  • HPLC
    • Each lab is equipped with an analytical HPLC
    • Multiple prep-HPLC systems for difficult purifications
    • QC systems with dual wavelength and PDA UV detectors
    • Chiral HPLC
  • Symphony Peptide Synthesiser (Protein Technologies, Inc.)
  • MBraun Solvent purifier for high quality reaction solvents
  • Grace Reveleris Flash Chromatography system (Dual UV detectors coupled with an evaporative light scattering detector for optimum purity)
  • CEM Discover Microwave reactor, Resonance 521 Microwave reactor
  • Each lab is equipped with Buchi R-205 rotavapors and Edwards RV8 vacuum pumps

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Related research

Areas of interest

  • Chemistry methodology and techniques, with specific application to halogenation and radiochemistry
  • Incorporation of 18F and 11C onto small molecules proteins and peptides
  • Investigation of methodologies to improve radiochemical outcomes, decreased reaction time, increased reaction efficiency
  • Automated synthesis and purification for improved reproducibility and safety
  • Development of novel macrocycles and chelation technologies for simple and rapid radiolabeling of small molecules, peptides, proteins and cells with radiometals for imaging and therapy.

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