Netupitant

CAT#: H205981

CAS#: 290297-26-6

Description: Netupitant is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity. Netupitant competitively binds to and blocks the activity of the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV).

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Synthetic Routes

Netupitant - Synthetic Route 1

Netupitant route01

Synthetic reference

Hoffmann-Emery, Fabienne; Hilpert, Hans; Scalone, Michelangelo; Waldmeier, Pius. Efficient Synthesis of Novel NK1 Receptor Antagonists: Selective 1,​4-​Addition of Grignard Reagents to 6-​Chloronicotinic Acid Derivatives. Journal of Organic Chemistry. Volume 71. Issue 5. Pages 2000-2008. Journal. (2006).

Netupitant - Synthetic Route 2

Netupitant route02

Synthetic reference

Wang, Qiang; Cao, Kangping; Xie, Yipeng; Gu, Xin; Zhou, Xinyu; He, Xiao Assignee Sichuan Hairong. Process for the preparation of netupitant. Assignee Sichuan Hairong Pharmaceutical Co., Ltd., Yangtze River Pharmaceutical Group, Peop. Rep. China; Sichuan Haihui Pharmaceutical Co., Ltd. CN 107698500. (2018).

Netupitant - Synthetic Route 3

Netupitant route03

Synthetic reference

Kovi, Ravishanker; Kannapan, Jayaraman; Thakor, Sanjay F.; Naik, Ashish. Process for the preparation of netupitant, pharmaceutically acceptable salts and intermediates thereof. Assignee Apicore US LLC, USA. US 20150315149. (2015).