The economic relevance of resistance building among agronomically important weeds against multiple herbicide classes has become widely accepted during the last five to ten years. In consideration of this fact, it is generally understood that new chemistries addressing unprecedented modes of herbicide action are urgently needed for the development of future weed control solutions.  As part of our early phase program, the aminoisothiazoles, a new class of herbicides displaying a new mode of action, were discovered and provided interesting biological efficacy.<br/>Several new chemistries were developed in order to fully explore this class<sup>1),2),3),4)</sup>.  For example, despite being unprecedently reported in the literature, the C-4 functionalization of 3-aminoisothiazole derivatives was done using halogen-magnesium exchange and quenching with various electrophiles. Several non-commercial amines were also prepared to broaden the scope of the amide part at the C-5 position of the isothiazole. To access such amines, selective chlorination or decarboxylative fluorination were for example successfully accomplished.

Chemistry behind the aminoisothiazoles: A new class of herbicides

256th National Meeting (2018)

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