Title: The Design and Synthesis of a Herbicide Targeted Library of N-[1-(1,3- Benzoxazol-2-yl)Alkyl]-6-Alkyl-1,3,5-Triazine-2,4-Diamines
Volume: 8
Issue: 7
Author(s): Hansjorg Dietrich, Wolfgang Giencke and Robert Klein
Affiliation:
Keywords:
solid phase synthesis, irori technology, parallel synthesis, herbicides, benzoxazoles, diversity analysis, physicochemical properties, library design
Abstract: Amino acids were immobilised by attaching them via a carbamate linker to Wang resin. These intermediates were converted to1-(1,3-benzoxazol-2-yl)alkanamines over three steps, followed by coupling with 4-alkyl-6-chloro-1,3,5-triazine-2-amines to furnish the desired N-[1-(1,3-benzoxazol-2-yl)alkyl]-6-alkyl- 1,3,5-triazine-2,4-diamines. Physico-chemical property profiles were used to support design and development of a combinatorial library. The synthetic methodology described herein was validated with the production of a herbicide targeted library of 300 members.