Synthesis of Commercial Phosphodiesterase(V) Inhibitors

@inproceedings{Dunn2005SynthesisOC,
  title={Synthesis of Commercial Phosphodiesterase(V) Inhibitors},
  author={Peter James Dunn},
  year={2005}
}
  • Peter James Dunn
  • Published 2005
  • Chemistry
    • 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. 
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    Development on the Synthesis of Phosphodieseterase Type 5 (PDE5) Inhibitors

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    CITES BACKGROUND

    Synthesis of isotope – labeled selective PDE5 inhibitor sildenafil (UK 92480-10)

    An overview of the synthetic routes to the best selling drugs containing 6-membered heterocycles

    Discovery of novel pyrazolopyrimidinone analogs as potent inhibitors of phosphodiesterase type-5.

    Alternative method for the synthesis of imidazo[5,1-f][1,2,4]triazin-4(3H)-one—a substrate for the preparation of phosphodiesterase (5) inhibitors

    Regioselective multi-component synthesis of 1H-pyrazolo[3,4-d]pyrimidine-6(7H)-thiones

    Improved synthesis of tadalafil using dimethyl carbonate and ionic liquids

    Accelerating the semisynthesis of alkaloid-based drugs through metabolic engineering.

    Characterization of Sildenafil analogs by MS/MS and NMR: a guidance for detection and structure elucidation of phosphodiesterase-5 inhibitors.

    Cyclization of 5-amino-1-aryl-1H-pyrazole-4-carbonitriles with β-dicarbonyl compounds

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    Chinese Patent CN 99 - 111153 ,

    • D. Yang, H. Wang, H. Shi
    • 2001

    World Patent , WO 04 / 011463 . Scheme 14 . Building blocks for tadalafil Scheme 15

    • M. W. Orme, J. C. Sawyer, M. J. Martinelli, C. W. Doecke, J. M. Pawlak