Our flow reactor range has already been established in the top 4 agrochemical companies globally at being able to improve a number of previously restricted reactions such as hydrogenation, oxidation or ozonolysis. However, the search for new heterocycles to discover new pesticides or herbicides is of the utmost importance. Below you can find some examples of how our flow reactor range can help you in making novel molecules or improving synthesis routes.

Hydrogenation of heterocycles to produce novel compounds

It has already been well established that the H-Cube series systems make significant advances for hydrogenation in terms of safety, speed and capabilities. To generate new molecules, the high-pressure capability (100 bar, 1450 psi) of the instrument can be utilized, coupled with short residence times in order to selectively reduce a heterocycle and by this, to dramatically alter its properties. The main advantage of this method is that you can use chemical material that is currently available to you from your stock. This means compounds could be tested quickly and cheaply.

Novel heterocycles using high temperature synthesis

Heterocyclic carbonyl compounds e.g. quinolones, pyridopyrimidinones, naphthyridinones are important structural motifs in various biological active compounds (e.g. norfloxacin, nalidixic acid). One of the most practical approaches for their synthesis is the thermal cyclisation of the appropriate open chain intermediates. Such molecules can be derived either from a condensation product of formaldehyde acetal and a CH-acidic methylene containing precursor, or cyano-acetic acid ester in Gould-Jacobs reaction. Using this method with the Phoenix Flow Reactor™ at 300°C and high pressure, a series of bicyclic compounds can be generated and novel heterocyclic scaffolds can be made in this manner very effectively and quickly.

Please also see our application note here.