Nintedanib

CAT#: H200496

CAS#: 656247-17-5

Description: Nintedanib, also known as BIBF 1120, is an orally bioavailable inhibitor of vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet derived growth factor receptor (PDGFR). Intedanib selectively binds to and inhibits vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet-derived growth factor receptor (PDGFR) tyrosine kinases, which may result in the induction of endothelial cell apoptosis; a reduction in tumor vasculature; and the inhibition of tumor cell proliferation and migration.

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Synthetic Routes

Nintedanib - Synthetic Route 1

Nintedanib route01

Synthetic reference

Roth, Gerald J.; Heckel, Armin; Colbatzky, Florian; Handschuh, Sandra; Kley, Jorg; Lehmann-Lintz, Thorsten; Lotz, Ralf; Tontsch-Grunt, Ulrike; Walter, Rainer; Hilberg, Frank. Design, Synthesis, and Evaluation of Indolinones as Triple Angiokinase Inhibitors and the Discovery of a Highly Specific 6-​Methoxycarbonyl-​Substituted Indolinone (BIBF 1120). Journal of Medicinal Chemistry. Volume 52. Issue 14. Pages 4466-4480. Journal. (2009).

Nintedanib - Synthetic Route 2

Nintedanib route02

Synthetic reference

Edupuganti, Ramakrishna; Taliaferro, Juliana M.; Wang, Qiantao; Xie, Xuemei; Cho, Eun Jeong; Vidhu, Fnu; Ren, Pengyu; Anslyn, Eric V.; Bartholomeusz, Chandra; Dalby, Kevin N. Discovery of a potent inhibitor of MELK that inhibits expression of the anti-​apoptotic protein Mcl-​1 and TNBC cell growth. Bioorganic & Medicinal Chemistry. Volume 25. Issue 9. Pages 2609-2616. Journal; Online Computer File. (2017).

Nintedanib - Synthetic Route 3

Nintedanib route03

Synthetic reference

Arava, Veerareddy; Gogireddy, Surendrareddy. An improved process for the synthesis of nintedanib esylate. Synthetic Communications. Volume 47. Issue 10. Pages 975-981. Journal; Online Computer File. (2017).

Nintedanib - Synthetic Route 4

Nintedanib route04

Synthetic reference

Li, Zeng; Cheng, Xiaosong; He, Xianliang; Zhang, Jicheng; Huang, Luning; Tao, Anping; Gu, Hong. Method for preparing Nintedanib and intermediate thereof. Assignee Shanghai SynCores Technologies, Inc., Peop. Rep. China. CN 107935908. (2018).

Nintedanib - Synthetic Route 5

Nintedanib route05

Synthetic reference

Arava, Veera Reddy; Gogireddy, Surendrareddy; Jasti, Venkateswarlu. Preparaton of a nintedanib ethanesulphonate polymorph, processes and novel intermediates thereof. Assignee Suven Life Sciences Limited, India. IN 2015CH02307. (2016).

Nintedanib - Synthetic Route 6

Nintedanib route06

Synthetic reference

Ji, Min; Chen, Hao; Cai, Jin; Liu, Haidong; Li, Rui. Preparation of Nintedanib and its intermediate. Assignee Southeast University, Peop. Rep. China. CN 105837493. (2016).

Nintedanib - Synthetic Route 7

Nintedanib route07

Synthetic reference

: Rao, Tadimeti; Zhang, Chengzhi. Preparation of deuterated nintedanib as inhibitors of tyrosine kinase. Assignee Auspex Pharmaceuticals, Inc., USA. US 20150284327. (2015).

Nintedanib - Synthetic Route 8

Nintedanib route08

Synthetic reference

Xu, Xuenong. Simple and green method for preparation of nintedanib. Assignee Suzhou Miracpharma Technology Co., Ltd., Peop. Rep. China. CN 104262232. 2015