Telaprevir (VX-950), marketed under the brand names Incivek and Incivo, is a pharmaceutical drug for the treatment of hepatitis C co-developed by Vertex Pharmaceuticals and Johnson & Johnson. It is a member of a class of antiviral drugs known as protease inhibitors. Specifically, telaprevir inhibits the hepatitis C viral enzyme NS3.4A serine protease. Telaprevir is only indicated for use against hepatitis C genotype 1 viral infections and has not been proven to have an effect on or being safe when used for other genotypes of the virus. The standard therapy of pegylated interferon and ribavirin is less effective on genotype 1.
Moni, Lisa; Banfi, Luca; Basso, Andrea; Carcone, Luca; Rasparini, Marcello; Riva, Renata. Ugi and Passerini Reactions of Biocatalytically Derived Chiral Aldehydes: Application to the Synthesis of Bicyclic Pyrrolidines and of Antiviral Agent Telaprevir. Journal of Organic Chemistry. Volume 80. Issue 7. Pages 3411-3428. Journal; Online Computer File. (2015).
Znabet, Anass; Polak, Marloes M.; Janssen, Elwin; de Kanter, Frans J. J.; Turner, Nicholas J.; Orru, Romano V. A.; Ruijter, Eelco. A highly efficient synthesis of telaprevir by strategic use of biocatalysis and multicomponent reactions . Chemical Communications (Cambridge, United Kingdom). Volume 46. Issue 42. Pages 7918-7920. Journal. (2010).
Zhang, Fan; Wen, Xiaoan; Xu, Qing-Long; Sun, Hongbin. Asymmetric synthesis of 3,4-disubstituted proline derivatives: Application in synthesis of hepatitis C virus protease inhibitor telaprevir. European Journal of Organic Chemistry. Volume 2014. Issue 36. Pages 8101-8109. Journal. (2014).
Anon. Process for the preparation of telaprevir and intermediates thereof. IP.com Journal. Volume 14. Issue 1B. Pages 1-6. Journal; Patent. (2014).
Sun, Guodong; Chen, Zongming; Zhang, Dexi; Chen, Yonghao. Method for preparing drug for treatment of hepatitis C. Assignee Sunshine Lake Pharma Co., Ltd., Peop. Rep. China. CN 104558106. (2015).
Barth, Roland; Benito-Garagorri, David; Wilhelm, Thorsten. Process for the preparation and isolation of (S)-3-amino-N-cyclopropyl-2,2-dialkoxyhexanamide and (S)-tert-butyl [1-(cyclopropylamino)-2,2-dialkoxy-1-oxohexan-3-yl]carbamate via novel cyclic anhydrides and use thereof for the preparation of telaprevir. Assignee Sandoz AG, Switz. WO 2015036522. (2015).
Kumar, Satish; Durvasula, Venugopal Venkatarama; Rathod, Parendu Dhirajlal; Aryan, Ram Chander. Process for the preparation of telaprevir and intermediates. Assignee Ranbaxy Laboratories Limited, India. WO 2014203208. (2014).
Nandi, Sukumar; Sivakumaran, Meenakshisunderam. An improved process for the preparation of Telaprevir. Assignee Aurobindo Pharma Ltd., India. IN 2012CH04278. (2014).
Chen, Youjin; Pan, Junfeng; Ma, Yaping; Yuan, Jiancheng. Process for preparation of telaprevir. Assignee Hybio Pharmaceutical Co., Ltd., Peop. Rep. China. CN 103554224. (2014).
Li, Jinliang; Zhao, Nan; Ge, Ruijuan. Process for preparation of telaprevir and intermediates thereof. Assignee Shanghai Desano Pharmaceutical Co., Ltd., Peop. Rep. China; Shanghai Desano Chemical. CN 103570605. (2014).
