New methods of synthesizing new compounds and new molecules are rapidly evolving, and more and more new technologies are emerging in the field of drug discovery. A right route is the key to ensuring the rapid development and supporting drug discovery project. A viable synthetic route is also required to meet all requirements, such as scalability, repeatability and cost reduction.

Route Scouting and Development

Creative Biolabs provides route scouting and development service. Our panel of experts is looking for the most effective and cost-effective route to synthesize existing compounds or generic active ingredients regardless of whether the compound is already described in the literature, or designing new chemical entities by finding brand new chemical route. A viable route at Creative Biolabs requires:

  • Apply innovation such as biocatalysis, chemocatalysis, and flow systems in the route
  • Reduce number of reaction steps for key intermediates
  • Reduce the number of steps for key intermediates
  • Decrease the timeline for scale up
  • Decrease the cost of API

There are many adjustment and improvement options for route scouting and development:

  • Changing solvents: When considering the reaction route, several issues should be addressed. For example, in the synthesis of (S)-2-({3-[(S)-5-chloro-1-(4-chloro-phenyl)indan-1-yl]propyl}methylamino)propionic acid, the strategy for route scouting and process development is based on a short synthesis and SMB resolution of a key chiral intermediate for the introduction of one of the two stereocenters. And the main concern during scale-up of the synthesis is the safety of the step to incorporate sodium dimsylate (the sodium salt of DMSO) and this problem is solved by using THF as a safety solvent in the largescale process.
  • Crystallizing: Crystallisation has the potential to be a useful purification technique and many crystal structures are stable. Crystal formation can be achieved by various methods, such as: cooling, evaporation, addition of a second solvent to reduce the solubility of the solute, solvent layering, sublimation, changing the cation or anion, as well as other methods. Variation in cooling time, agitation and perhaps surfactants can all be employed to alter crystal size.
  • Telescoping: Telescoping is the procedure whereby the product of a chemical reaction is not isolated but is used directly in the next stage of synthesis, often as a solution of the product. Advantages include that it can improve time-efficiency and it can be used to handle non-crystalline oily products and avoid intermediates that are toxic, irritant, and odorous or of unknown toxicological properties.

Creative Biolabs' experience in the chemical synthesis research and custom synthesis of complex molecules has laid the foundation for our ability to find new and better molecular synthesis routes. We will help you improve process efficiency with the latest and most optimized technology choices. If you are interested in our innovative route scouting and development services, please do not hesitate to contact us.

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