RESUMO
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.
Assuntos
Agroquímicos/química , Técnicas de Química Combinatória/métodos , Agroquímicos/síntese química , Antifúngicos/síntese química , Antifúngicos/química , Disponibilidade Biológica , Desenho Assistido por Computador , Herbicidas/síntese química , Herbicidas/química , Inseticidas/síntese química , Inseticidas/química , Bibliotecas de Moléculas Pequenas , Relação Estrutura-AtividadeRESUMO
[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.