Transforming Discovery into Opportunity

Medicinal Chemistry

Head, James Jaquith, PhD (bio)

The central goal of drug discovery is identifying and producing chemical entities (i.e. drugs). These chemical compounds can be used in the treatment or diagnosis of disease as well as helping to elucidate and to understand the disease process. Most orally and parenterally delivered drugs are small molecules and peptides and these typically have molecular weights.


The Medicinal Chemistry Division applies modern synthetic methods and principles to design and synthesize novel compounds for biological evaluation as potential drugs. The chemical compounds produced are optimized in an iterative process of synthesis followed by evaluation in a battery of assays to produce a clinical candidate with appropriate pharmacological, pharmacokinetic and toxicological properties. The Medicinal Chemistry Division also synthesizes reference compounds, modified drugs for improved drug delivery (pro-drugs), specialized excipients for drug delivery, specialized reagents for the modification targets of biological origin, radiolabeled compounds, larger GLP batches of development candidates for pre-clinical toxicology and formulation studies.

Capabilities and Expertise
  • Medicinal Chemistry:
  • Rational drug design and synthesis of analogs
  • Library synthesis (automated platform)
  • Targeted structure-activity relationships
  • Lead optimization
  • Process Chemistry:
  • Optimization of synthetic routes for the efficient and safe scale-up of drug substances (process optimization)
  • Scale up synthesis and analysis
  • Preparation of tech-transfer packages, SOPs and batch records
  • Custom Synthesis:
  • Design, planning, optimization and scale-up of custom chemicals
  • Equipment:
  • High-field multidimensional multinuclear NMR (400 and 600 MHz)
  • Walk-up electro-spray LCMS
  • Automated robotic synthesis (ChemSpeed)
  • Semi-automated microwave synthesis (Biotage and CEM)
  • Computer aided drug design
  • Asymmetric synthesis and analysis
  • Large-scale chemical reactors and evaporation (up to 22 L process reactors, 30 L rotovap)
  • Automated flash purification (Biotage)
  • Parr hydrogenators (0.5 and 2.5 L)

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