Medicinal Chemistry & Chemical Biology, Contributed Talk (15min)

The Discovery of Isocycloseram: a Novel Isoxazoline Insecticide

M. El Qacemi1
1Syngenta Crop Protection

Isocycloseram is a novel insecticide discovered at Syngenta Crop Protection. It is a member of the isoxazoline class of insecticides, which acts as a non-competitive antagonist of the invertebrate GABA receptor at a site distinct to that of fiproles and cyclodienes, resulting in excellent efficacy against invertebrate pests.

Innovative approaches for the delivery of modern agrochemicals such as multi-parameter optimization and faster cycles of Design-Synthesis-Test-Analysis (DSTA) were implemented during the research phase on the isoxazoline insecticidal class and led us to the discovery of Isocycloseram. The synthesis, optimization and biological efficacy aspects of this new chemical class will be presented.

[1] The discovery of isocycloseram: A novel isoxazoline insecticide in Recent Highlights in the Discovery and Optimization of Crop Protection Products. Jérôme Cassayre*, Tomas Smejkal, Judith Blythe, Patrik Hoegger, Peter Renold, Thomas Pitterna, C.S. Prasanna, Helmars Smits, Edouard Godineau, Torsten Luksch, Guillaume Berthon, Girish Rawal, Rupesh Patre, Mukul Lal, Mohamed Boussemghoune, Simonetta Masala, Fabien Barreteau, Michael Flaeschel, Juliane Vogt and Myriem El Qacemi*. Editor(s): Peter Maienfisch, Sven Mangelinckx, Academic Press2021, Pages 165-212,