A safe and practical method for the preparation of 7α-thioether and thioester derivatives of spironolactone

  title={A safe and practical method for the preparation of 7$\alpha$-thioether and thioester derivatives of spironolactone},
  author={G. Agusti and S. Bourgeois and N. Cartiser and H. Fessi and M. B. Borgne and Thierry Lomberget},
Spironolactone is a renal competitive aldosterone antagonist. One of its most important metabolite is the 7α-methylthio spironolactone: thus it is very important to have an efficient and safe access to this compound, for pharmacokinetic studies. In this context, we synthesized this metabolite by thioalkylation of 7α-thio spironolactone using Hünig's base with a very good yield. We also used our procedure to prepare, with an easy work-up and high yields, 7α-thioether and thioester derivatives of… Expand

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