Riociguat

CAT#: H503750

CAS#: 625115-55-1

Description: Riociguat, also known as BAY 63-2521, is a novel drug that is currently in clinical development by Bayer. It is a stimulator of soluble guanylate cyclase (sGC). At the moment Phase III clinical trials investigate the use of riociguat as a new approach to treat two forms of pulmonary hypertension (PH): chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH). Riociguat constitutes the first drug of a novel class of sGC stimulators.

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Synthetic Routes

Riociguat - Synthetic Route 1

Riociguat route01

Synthetic reference

: Follmann, Markus; Ackerstaff, Jens; Redlich, Gorden; Wunder, Frank; Lang, Dieter; Kern, Armin; Fey, Peter; Griebenow, Nils; Kroh, Walter; Becker-Pelster, Eva-Maria; Kretschmer, Axel; Geiss, Volker; Li, Volkhart; Straub, Alexander; Mittendorf, Joachim; Jautelat, Rolf; Schirok, Hartmut; Schlemmer, Karl-Heinz; Lustig, Klemens; Gerisch, Michael; Knorr, Andreas; Tinel, Hanna; Mondritzki, Thomas; Truebel, Hubert; Sandner, Peter; Stasch, Johannes-Peter. Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure. Journal of Medicinal Chemistry. Volume 60. Issue 12. Pages 5146-5161. Journal; Online Computer File. (2017).

Riociguat - Synthetic Route 2

Riociguat route02

Synthetic reference

Li, Liang; Li, Xingzhou; Liu, Yadan; Zheng, Zhibing; Li, Song. Synthesis of riociguat in treatment of pulmonary hypertension. Zhongguo Yaowu Huaxue Zazhi. Volume 21. Issue 2. Pages 120-125. Journal. (2011).

Riociguat - Synthetic Route 3

Riociguat route03

Synthetic reference

Nerkararyan, Kristine; Sargsyan, Karine; Gasparyan, Nairi; Gharibyan, Mariam; Movsisyan, Mikayel; Porstmann, Frank. 2-​[benzyl(methyl)​amino]​propanedinitrile-​new building block for synthesis of Riociguat, a pulmonary hypertension drug. Pharma Chemica. Volume 10. Issue 6. Pages 62-66. Journal; Online Computer File. (2018).

Riociguat - Synthetic Route 4

Riociguat route04

Synthetic reference

Lu, Zhaoli; Li, Yuxing; Zhang, Hongyan; Yan, Xiongwei. A multi-​step synthesis of heterocyclic organic compound: inhibiting growth of human osteogenic sarcoma cells. Latin American Journal of. Pharmacy. Volume 37. Issue 1. Pages 139-143. Journal. (2018).

Riociguat - Synthetic Route 5

Riociguat route05

Synthetic reference

: Yu, Libing; Guo, Maojun; Yang, Qingang; Ji, Changyou. Process for preparation of Riociguat intermediate pyrazolo[3,4-b]pyridine compound. Assignee Alputon Inc., Peop. Rep. China; Shanghai Acebright Pharmaceuticals Group Co., Ltd. CN 105777743. (2016).