[Orb Pilot Scale up Reactor: Image from Syrris]
Flow chemistry techniques are increasingly being used in drug discovery to provide cost-effective access to a wide range of structurally diverse small molecule analogs, as well as access to previously underused or inaccessible chemistries. There are several ways that this powerful technique can be used to increase structural diversity when building candidate molecules, including linear progression from diverse starting materials, multicomponent reactions around core structural motifs, synthesis of uncommon low diversity starting material sub-sets, and convergent synthesis approaches. The diversity of the starting components is a key consideration when deciding the most suitable strategy for each specific application, but the development of automated, modular flow chemistry systems has made all these approaches far easier to achieve. Here we outline the various methods and…Realizing the potential of flow chemistry in hit to leads
Flow chemistry image courtesy of Vernalis Research
Flow chemistry is a growing technology in the pharma industry, where it has proved itself invaluable, especially in the process development phase of drug discovery. However, the hit-to-lead generation phase of drug discovery has been slower to embrace these techniques. Nevertheless, the potential benefits are huge, particularly for rapid library generation and challenging chemistries that were previously hard to achieve by traditional batch methods. This article looks at how finding a groundbreaking flow chemistry application led to the wider adoption of flow chemistry in synthesis at a small pharma company.
The pharma industry frequently collaborates with CROs and smaller technology companies in the lead generation phase of drug discovery, adopting a medicinal chemistry approach to the development, synthesis and analysis of drug molecules and other bioactiv…