Crop Protection Chemistry: Innovation with Purpose

Applications of Isosteres of Piperazine in the Design of Biologically Active Compounds: Part 2

“…Evolution in this direction brings into focus new opportunities within chemical space that have thus far largely been uncharted in crop protection because of cost and manufacturing limitations. A requirement for a reduced amount of product allows for the exploration of more diverse and complex chemistry that can meet more stringent performance, safety, and sustainability criteria while continuing to reduce the cost of application per hectare . As a result, agricultural chemicals are increasing in complexity and approaching that of drug candidates. − Examples that illustrate this trend include cyclobutrifluram ( 272 ), an inhibitor of the mitochondrial succinate dehydrogenase (SDH) in nematodes, isocycloseram ( 273 ), a modulator of the insect γ-aminobutyric acid (GABA)-gated chloride channels, and insecticide and acaricide spiropidion ( 274 ), a procide of the active acetyl-CoA-carboxylase-inhibiting principle. − …”

“…82 Homologous (3-azabicyclo[3.1.0]hexan-6-yl)methanamine (160) has found application as a piperazine mimic, notably in the ATX inhibitor 117, but also has utility as a scaffold in drug design that extends beyond the aspect of simple piperazine bioisosterism to a broader mimicry of diamines. This is exemplified by the Gly-T inhibitor PF-03463275 ( 161), the T-type calcium channel inhibitor MIL 218 (162), and the 5HT 4 partial agonist 163. 84−86…”

Use of Renewable Resources Towards the Sustainable Production of Crop Protection Agents

“…We are actively pursuing a science-based approach to the sustainable design of new ingredients. [73] Onboarding renewable feedstocks into the design of active ingredients is increasingly appearing as demonstrated by the synthesis of thiametoxam analogs from the available natural product Nootkatone. [74] Such an aim is a clear objective on our strategic agenda and we are intensifying our efforts in this direction.…”

A case study in green chemistry: the reduction of hazardous solvents in an industrial R&D environment

“…1 Accelerating innovation in crop protection to meet food demand and help farmers to become more resilient to the consequences of climate change while limiting its causes is a great global challenge for the next decade. 2 The targeted profile of new active ingredients in crop protection has significantly evolved in the last 20 years to reflect this sustainability challenge and respond to grower needs, more stringent regulatory criteria and legitimate society expectations. A crop protection chemist today has the challenging but exciting task to design and prepare compounds which:…”

“…Accelerating innovation in crop protection to meet food demand and help farmers to become more resilient to the consequences of climate change while limiting its causes is a great global challenge for the next decade. 2…”