There are two major reasons for the fundamental value of heterocycles for the lead optimisation of agrochemicals. The heterocyclic scaffold of an agrochemical often has a positive impact on its synthetic accessibility and its physicochemical properties, determining uptake and bioavailability. In addition, heterocycles seem to be perfect bioisosteres of other isocyclic or heterocyclic rings as well as of several different functional groups, leading in many cases to better biological activity. Recently, some unique heterocyclic ring closure reactions have been found to be valuable tools for the synthesis of examples from the modern fungicide classes of succinate dehydrogenase inhibitors and tubulin polymerisation promoters. Such applications of heterocyclisations to current crop protection chemistry will be reported in the lecture.

Significance of heterocycles for agrochemicals: Current examples from fungicide research

244th National Meeting (2012)

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