Active Pharmaceutical Ingredients (Api): Synthesis and Analysis

Active Pharmaceutical Ingredients (Api): Synthesis and Analysis



Learning outcomes

To provide information and knowledge on practical active pharmaceutical ingredients (API) industrial synthesis. The focus will be on API industrial synthesis (route discovery and selection, hazards and process development) and characterization (methods and specifications). Integration with industrial property (patents).


I Synthetic route discovery and selection

  • The evolution of chemical synthesis from laboratory to industrial scale.
  • Lab versus Industrial synthesis.
  • Organic drug synthesis The ideal process.
  • Synthetic route discovery and selection. Patents.

II Hazards in industrial synthesis

  • Major areas: toxicity, fire/explosion and chemical reaction Major accident causes.
  • Hazards in process development and scale-up. Process safety.
  • Thermal hazards: thermal stability and explosiveness of compounds and mixtures.
  • Gas generation. Process abnormalities.

III Process Development and scale-up (batch)

  • Main strategy: individual step study, integration of individual steps and global.
  • Individual step development: the chemical transformation, the work-up, the isolation and purification of the product. Polymorphism and chiral synthesis.

IV Analysis

  • In-process control and API characterization.
  • Polymorphism, enantiomeric.
  • API stability and specifications.