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Review | Special issue | Vol 101, No. 2, 2020, pp.373-382
Published online, 7th August, 2019
DOI: 10.3987/REV-19-SR(F)2
Mini-Review: The Chemistry of Vorapaxar – Is There Any Room for Improvement Left?

Piotr P. Graczyk* and Sven Nerdinger

*Selvita Services Sp. z o. o., Bobrzynskiego 14, 30-348 Krakow, Poland


Based on the case of Vorapaxar, this review describes the key role of an early chemistry effort to enable rapid discovery of an optimal synthetic route to a commercially important product. The intramolecular Diels-Alder (IMDA) reaction developed by scientists from Schering to make natural product Himbacine in mid-‘90s allowed formation of the Vorapaxar’s backbone almost 10 years later. Since then this strategy has been followed by all companies. Additional improvements by Schering to the synthesis of Vorapaxar greatly limited the opportunities for generic manufacturers to secure new intellectual property. Most of the chemistry presented in this review comes from the patent applications and as such has not been subjected to rigorous peer review, but in our opinion this paper may serve as helpful information for readers in the area of drug discovery.