Recent advances in flow chemistry using equipment such as the new Vapourtec R-4 flow reactor heater can significantly speed up drug discovery and lead generation. The ability to carry out a reaction and simply collect a pure compound makes flow chemistry a particularly attractive option in drug discovery and process development where reaction optimisation and scale-up are very important.
The unit can hold four reactors, either tubes for homogenous reactions or columns for heterogeneous reactions, and cope with volumes between 0.2ml and 15ml. All four reactors can be heated simultaneously with independently set temperatures, by a unique heating system. Reactor cartridges can be switched simply and quickly depending on the application.
One of the most exciting things about the product is that the glass heat exchangers ensure the entire working volume of the reactor is visible at all times - this is particularly important when using superheated solvents that may form gas bubbles that lead to product precipitation or simply for observing colour changes during reaction.
Reagents may either be mixed as liquids or a reagent may be passed through a column of immobilised reagent or a catalyst. The products are eluted at the end of the reaction often without the need for any purification. By incorporating real-time analysis techniques, rapid optimisation and excellent quality control can be achieved.
Talking to LabTechnologist.com Duncan Guthrie, director at Vapourtec, said: "the majority of interest in the apparatus has been due to the ease of predictable scale-up, where comparable yields can be obtained even when a reaction is scaled-up by factors of over 100 to 100g."
This sort of scale-up can cause no-end of problems in a more conventional batch-type process, where yields can drop significantly after only scaling up by a factor of 10.
Recent advances have been made in the field of flow chemistry at the University of Cambridge by Professor Steven Ley and co-workers, where individual steps of a multi-step synthesis can be linked together allowing one reaction to flow into the next. Earlier this year the Ley group published the first multi-step flow through preparation of a natural product, oxomaritidine.
Increasing the speed of access to drug targets using these techniques will allow more rapid interrogation and probing of how these targets behave in biological systems, potentially expediting the decision-making processes in lead generation and drug design.