ABSTRACT
Combinatorial chemistry and high throughput screening have had a profound effect upon the way in which agrochemical companies conduct their lead discovery research. The article reviews recent applications of combinatorial synthesis in the lead discovery process for new fungicides, herbicides and insecticides. The role and importance of bioavailability guidelines, natural products, privileged structures, virtual screening and X-ray crystallographic protein structures on the design of solid- and solution-phase compound libraries is discussed and illustrated.
Subject(s)
Agrochemicals/chemistry , Combinatorial Chemistry Techniques/methods , Agrochemicals/chemical synthesis , Antifungal Agents/chemical synthesis , Antifungal Agents/chemistry , Biological Availability , Computer-Aided Design , Herbicides/chemical synthesis , Herbicides/chemistry , Insecticides/chemical synthesis , Insecticides/chemistry , Small Molecule Libraries , Structure-Activity RelationshipABSTRACT
[reaction: see text] A stepwise [3+3] annelation sequence to tetrahydropyridines via addition of the Büchi Grignard to aziridines has been developed. These intermediates can be further functionalized with good regio- and stereocontrol and this methodology has been employed in the stereoselective formal synthesis of (-)-dihydropinidine.
