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Development of NK3R Antagonists with a Degradable Scaffold in the Natural Environment: Synthesis and Application of Fused Piperazine Derivatives for Investigation of Degradable Core Motifs

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Abstract

For investigation of decomposable scaffolds for the fezolinetant triazopiperazine core in the natural environment, an efficient method for synthesis of [1,2,4]triazolo[4,3-a]piperazine derivatives was established based on gold(I)-catalyzed domino cyclization of an amidrazone substrate with a terminal alkyne. The amidoxime congeners were also converted into [1,2,4]oxadiazolo[4,5-a]piperazine derivatives in the presence of a gold catalyst.

Keywords

Gold-catalyst Domino cyclization Triazolopiperazine 

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Copyright information

© Springer Nature Singapore Pte Ltd. 2020

Authors and Affiliations

  1. 1.Graduate School of Pharmaceutical SciencesKyoto UniversityKyotoJapan

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