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

Authors

  • Jutta Glock
  • Peter D. J. Grootenhuis
  • Steven Bondy
  • Daniel D. Comer
  • Soan Cheng
  • Arthur Steiger
  • Martin Zeller
  • Grit Laue
  • Adrian Friedmann
  • Olivier Jacob
  • Mafalda Nina
  • Hans-Jürg Widmer
  • Klaus Kreuz
  • Julie E. Penzotti
  • Hans Brunner
  • James Allen
  • Thierry Niderman
  • Hans Ulrich Haas
  • Renold Chollet
  • Martin Eberle
  • Peter Renold
  • William Lutz
  • Jürg Ehrler
  • Marian Valentini
  • Markus Walti
  • Evelyne Sieger
  • Thomas Vettiger
  • G. Wayne Craig

DOI:

https://doi.org/10.2533/chimia.2008.23

Keywords:

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

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.

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Published

2008-02-27

Issue

Section

Scientific Articles