Lead-Discovery of bis-Aromatic Alkynes: A Novel Class of Herbicides

Abstract

The search for new active molecules with novel modes of action and desirable physical properties is an ongoing endeavour. This publication describes the follow-up chemistry of a biological hit discovered in the screening system of Novartis Crop Protection, the legacy agrochemical parent of Syngenta Crop Protection. This chemistry was optimized through classical synthetic methods and automated parallel synthesis with coverage of important physical properties such as lipophilicity or Clog P and solubility. Preliminary biological activity from the greenhouse and field data with symptomology is presented.

Keywords

• Agrochemicals
• Alkyne template
• Combinatorial chemistry
• Discovery
• Sonogashira coupling