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Solid Phase Synthesis of 1,2,4-Triazinan-3-ones

  • Yongping Yu
  • John M. Ostresh
  • Richard A. Houghten
Part of the American Peptide Symposia book series (APSY, volume 7)

Abstract

Solid-phase parallel synthesis is used worldwide to generate libraries of small organic compounds in order to accelerate the drug discovery process [1]. The focus of this field of research, which initially involved the synthesis of peptides and oligonucleotides, is now on the synthesis of small organic molecules on the solid-phase. Heterocycles, such as benzodiazepines, hydantoins, pyrrolidines, and bicyclic guanidines, have received special attention in combinatorial synthesis due to their biological interesting properties [2]. This strategy has permitted the synthesis of large numbers of heterocycles in a short time frame, enabling their use in high-throughput screening. Compounds containing the 1,2,4-triazine moiety are in use as pharmaceuticals, pesticides, herbicides etc. [3]. As part of our ongoing efforts directed toward the solid phase synthesis of small molecule and heterocyclic compounds and the generation of their combinatorial libraries [4], we report here an efficient method for the synthesis of l,2,4-triazinan-3-ones from resin-bound acylated amino acid amides.

Keywords

Heterocyclic Compound Secondary Amine Ongoing Effort Solid Phase Synthesis Short Time Frame 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

References

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Copyright information

© Springer Science+Business Media Dordrecht 2001

Authors and Affiliations

  • Yongping Yu
    • 1
  • John M. Ostresh
    • 1
  • Richard A. Houghten
    • 1
  1. 1.Torrey Pines Institute for Molecular StudiesSan DiegoUSA

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