Annulation Approach to Tetrahydro-1,2,4-triazinecarboxylate Esters

Silver-Catalyzed [3+3] Annulation of Glycine Imino Esters with Seyferth–Gilbert Reagent To Access Tetrahydro-1,2,4-triazinecarboxylate Esters: Y.-J. Huang, J. Nie, C. W. Cheung, J.-A. Ma
Synlett 2020, 31, DOI: 10.1055/s-0039-1690894


Phosphorylated azines are important structural motifs in a number of areas such as drug discovery, materials science and catalysis. Synthesis of stereo-defined chiral and selectively phosphorylated rings incorporating one or more nitrogen atoms is not a straightforward task. This issue has been addressed by a recent study reported by the group of Prof Jun-An Ma from Tianjin University (P. R. of China) who developed a novel strategy for accessing the title compounds.

Professor Ma said: “A novel class of phosphorylated tetrahydrotriazines, which would find use in drug discovery, were accessed via silver-catalyzed annulation based on readily available glycine imino esters and Seyferth–Gilbert reagent.”

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