Fetzer, C., Korotkov, V. and Sieber, S. (2018) Preparation of ClpX Inhibitory Compounds Useful for the Treatment of Multidrug-Resistant Staphylococcus aureus and Leukemia. PCT Int. Appl., WO 2018114965 A1 20180628.

has been cited by the following article:

• TITLE: Synthesis of Substituted Benzothiazepine Compounds with Medicinal Potential

  AUTHORS: Clare E. Gutteridge, Brett W. Sadowski, Stephen M. Hughes, J. Alan Friedlander, Leighton G. Rodrigo, Michael C. Baxter, Nathan C. Lorei, Jonathan E. Harrell, Michael T. O’Neil

  KEYWORDS: Benzothiazepine, Knoevenagel Condensation, Thio-Michael Addition, Benzylidene Indandione, 2-Aminothiophenol

  JOURNAL NAME: International Journal of Organic Chemistry, Vol.10 No.3, September 21, 2020

  ABSTRACT: A versatile synthetic approach toward a series of benzothiazepines with medicinal potential (for example, compound 1) that allows incorporation of structural variation at the three aromatic regions of the structure, and at the sulfur atom, was developed. Knoevenagel condensation of indan-1,3-diones with benzaldehydes, yielded 2-benzylidineindan-1,3-diones, which undewent thio-Michael addition and intramolecular imine formation upon reaction with 2-aminothiophenols, to produce the target benzothiazepines. Use of indan-1,3-diones, benzaldehydes or 2-aminothiophenols bearing further substitution enabled production of novel 5,11-dihydro-12H-benzo[b]indeno [1,2-e][1,4]thiazepin-12-one analogs 1 - 14, including compounds bearing substitution at novel positions within the scaffold.