PROPYLPHOSPHONIC ANHYDRIDE (T3P®)-MEDIATED THREE-COMPONENT SYNTHESIS OF HEXAHYDRODIBENZO[<i>b</i>,<i>e</i>][1,4]DIAZEPIN-1-ONE DERIVATIVES

Authors

  • Viktor Hazai Directorate of Drug Substance Development, Egis Pharmaceuticals Plc., P. O. Box 100, Budapest 1475, Hungary
  • Tímea Szabó Directorate of Drug Substance Development, Egis Pharmaceuticals Plc., P. O. Box 100, Budapest 1475, Hungary
  • Balázs Volk Directorate of Drug Substance Development, Egis Pharmaceuticals Plc., P. O. Box 100, Budapest 1475, Hungary
  • Mátyás Milen Directorate of Drug Substance Development, Egis Pharmaceuticals Plc., P. O. Box 100, Budapest 1475, Hungary

DOI:

https://doi.org/10.1007/5351

Keywords:

1, 5-benzodiazepines, nitrogen heterocycles, propylphosphonic anhydride (T3P®), three-component synthesis.

Abstract

In this work, the novel approach via propylphosphonic anhydride (T3P®)-promoted synthesis of 1,5-benzodiazepines from o-phenylenediamine,
5,5-dimethylcyclohexane-1,3-dione (dimedone), and aromatic aldehydes has been studied. The reaction conditions were optimized and the scope of the reaction was extended to various aromatic aldehydes. The synthesized compounds were obtained in reasonable to good yields.

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Published

2020-02-28

Issue

Vol. 56 No. 2 (2020)

Section

Short Communications