Welcome to Hodoodo Chemicals

Nilotinib

CAT#: H100952

CAS#: 641571-10-0

Description: Nilotinib, also known as AMN107, is a small-molecule tyrosine kinase inhibitor approved for the treatment of imatinib-resistant chronic myelogenous leukemia. Structurally related to imatinib, it was developed based on the structure of the Abl-imatinib complex to address imatinib intolerance and resistance. Nilotinib is a selective Bcr-Abl kinase inhibitor that is 10-30 fold more potent than imatinib in inhibiting Bcr-Abl tyrosine kinase activity and proliferation of Bcr-Abl expressing cells. Nolitinib was developed by Novartis and is sold under the trade name Tasigna.

Synthetic Routes

Nilotinib - Synthetic Route 1

Synthetic reference

Ueda, Satoshi; Su, Mingjuan; Buchwald, Stephen L. Completely N1-selective palladium-catalyzed arylation of unsymmetric imidazoles: application to the synthesis of nilotinib. Journal of the American Chemical Society. Volume 134. Issue 1. Pages 700-706. 2012.

Nilotinib - Synthetic Route 2

Synthetic reference

Breitenstein, Werner; Furet, Pascal; Jacob, Sandra; Manley, Paul William. Preparation of pyrimidinylaminobenzamides as inhibitors of protein kinases, in particular tyrosine kinases for treating neoplasm, especially leukemia. Assignee Novartis A.-G., Switz.; Novartis Pharma G.m.b.H. WO 2004005281. (2004).

Nilotinib - Synthetic Route 3

Synthetic reference

Pan, Xiaoyan; Lu, Wen; Li, Pengfei; Wang, Fang; Wang, Chen; Hu, Zhigang; Zhang, Jie. A novel and facile synthetic approach for tasigna. Medicinal Chemistry. Volume 8. Issue 5. Pages 985-989. 2012.

Nilotinib - Synthetic Route 4

Synthetic reference

Zhang, Jie; He, Langchong; Pan, Xiaoyan; Lu, Wen; Wang, Chen; Wang, Sicen; Li, Xiling. Process for preparation of Nilotinib. Assignee Xi'an Jiaotong University, Peop. Rep. China. CN 102321073. (2012).

Nilotinib - Synthetic Route 5

Synthetic reference

Chen, Yongjiang; Wang, Lihua; Zhou, Hong; Wang, Congzhan. Synthesis of nilotinib. Zhongguo Yiyao Gongye Zazhi. Volume 40. Issue 6. Pages 401-403, 411. 2009.

Nilotinib - Synthetic Route 6

Synthetic reference

Liu, Xuejun; Chen, Xiaodong; Hao, Lu; Wu, Feng. Preparation method of nilotinib. Assignee Shanghai Fuxingxingtai Pharmaceutical Technology Co., Ltd., Peop. Rep. China. CN 109666023. (2019).

Nilotinib - Synthetic Route 7

Synthetic reference

Kompella, Amala; Bhujanga Rao, Adibhatla Kali Satya; Rachakonda, Sreenivas; Gampa, Venugopala Krishna; Nannapaneni, Venkaiah Chowdary. Process for the preparation of nilotinib hydrochloride. Assignee Natco Pharma Limited, India. EP 2626355. (2013).

Nilotinib - Synthetic Route 8

Synthetic reference

Huang, Wei-Sheng; Shakespeare, William C. An efficient synthesis of nilotinib (AMN107). Synthesis. Issue 14. Pages 2121-2124. 2007.

Nilotinib - Synthetic Route 9

Synthetic reference

Yeori, Adi; Wang, Yanling; Li, Jie; Zhu, Jirang; Lifshitz-Liron, Revital; He, Xungui. Process for preparation of Nilotinib and intermediates. Assignee Teva Pharmaceutical Industries Ltd., Israel; Teva Pharmaceuticals USA, Inc. WO 2010060074. (2010).

Nilotinib - Synthetic Route 10

Synthetic reference

McKenna, Joseph; Shieh, Wen-Chung. Process for the synthesis of pyrimidine derivative. Assignee Novartis A.-G., Switz.; Novartis Pharma G.m.b.H. WO 2006135641. (2006).