Synthesis of Commercial Phosphodiesterase(V) Inhibitors

  title={Synthesis of Commercial Phosphodiesterase(V) Inhibitors},
  author={Peter James Dunn},
  journal={Organic Process Research \& Development},
  • P. Dunn
  • Published 6 January 2005
  • Chemistry
  • Organic Process Research & Development
The literature syntheses (including patents) of three commercial phosphodiesterase(V) (PDE5) inhibitors (sildenafil, vardenafil, and tadalafil) are reviewed with particular emphasis on large-scale manufacture. For each of these compounds, some impressive chemical development work has been reported. 

Figures and Tables from this paper

Development on the Synthesis of Phosphodieseterase Type 5 (PDE5) Inhibitors
Phosphodieseterase type 5 inhibitors are safe, efficacy and well tolerated in the treatment of erectile dysfunction and therefore widely used. In this paper, the various synthetic methods and
Synthesis of isotope – labeled selective PDE5 inhibitor sildenafil (UK 92480-10)
Abstract Sildenfil a vasodilating agent is a selective inhibitor of cyclic guanosine monophosphate – specific phosphodiesterase type 5 which is used for the treatment of male erectile dysfunction and
An overview of the synthetic routes to the best selling drugs containing 6-membered heterocycles
This review which is the second in this series summarises the most common synthetic routes as applied to the preparation of many modern pharmaceutical compounds categorised as containing a
Identification, synthesis, and characterization of potential genotoxic impurities of sildenafil citrate drug substance
Different process-related sulfonyl esters in sildenafil were identified, synthesized, and characterized by using various spectroscopic techniques like liquid chromatography-mass spectrometry (LCMS), mass, 1H NMR, and FT-IR, and these efforts to synthesize and characterize them effectively have proved to be beneficial.
An Efficient and General Method for the Stereodivergent Syntheses of Tadalafil-Like Tetracyclic Compounds
A clean and general DBU-catalyzed epimerization at C-12a position of the tadalafil-like tetracyclic compounds has been fully studied. In addition, by using this clean epimerization as the key step,


Chinese Patent CN 99 - 111153 ,
  • 2001
World Patent , WO 04 / 011463 . Scheme 14 . Building blocks for tadalafil Scheme 15