Neratinib Maleate

CAT#: H201470

CAS#: 915942-22-2

Description: Neratinib, also known as HKI-272 or PB272, is an orally available, irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity. Neratinib binds to the HER-2 receptor irreversibly, thereby reducing autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocket of the receptor.

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Synthetic Routes

Neratinib Maleate - Synthetic Route 1

Neratinib Maleate route01

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Neratinib Maleate - Synthetic Route 2

Neratinib Maleate route02

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Neratinib Maleate - Synthetic Route 3

Neratinib Maleate route03

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Neratinib Maleate - Synthetic Route 4

Neratinib Maleate route04

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Optimization of 6,7-Disubstituted-4-(arylamino)quinoline-3-carbonitriles as Orally Active, Irreversible Inhibitors of Human Epidermal Growth Factor Receptor-2 Kinase Activity; Tsou, Hwei-Ru; Overbeek-Klumpers, Elsebe G.; Hallett, William A.; Reich, Marvin F.; Floyd, M. Brawner; Johnson, Bernard D.; Michalak, Ronald S.; Nilakantan, Ramaswamy; Discafani, Carolyn; Golas, Jonathan; Rabindran, Sridhar K.; Shen, Ru; Shi, Xiaoqing; Wang, Yu-Fen; Upeslacis, Janis; Wissner, Allan; Journal of Medicinal Chemistry; Volume 48; Issue 4; Pages 1107-1131; Journal; 2005

Neratinib Maleate - Synthetic Route 5

Neratinib Maleate route05

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The Wittig-Horner reaction for the synthesis of neratinib; Gu, Ning; Yang, Jiabin; Wang, Peng; Li, Lushen; Chen, Yang; Ji, Min; Research on Chemical Intermediates; Volume 39; Issue 7; Pages 3105-3110; Journal; 2013

Neratinib Maleate - Synthetic Route 6

Neratinib Maleate route06

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Synthesis of neratinib; Chen, Feng; Zhang, Shengping; Wang, Peibei; Li, Yuezhen; Lai, Yisheng; Zhongguo Yiyao Gongye Zazhi; Volume 45; Issue 8; Pages 701-705; Journal; 2014

Neratinib Maleate - Synthetic Route 7

Neratinib Maleate route07

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Preparation of substituted quinolines as protein tyrosine kinase inhibitors for treating cancer; Wissner, Allan; Rabindran, Sridhar Krishna; Tsou, Hwei-Ru; Assignee Wyeth, John, and Brother Ltd., USA; 2005; Patent Information; Apr 21, 2005; WO 2005034955 A1

Neratinib Maleate - Synthetic Route 8

Neratinib Maleate route08

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A large-scale synthesis of 4-amino-2-butenoyl chlorides, useful as intermediates in preparation of [(dimethylaminocrotonyl)amido]quinoline derivatives; Considine, John Leo; Daigneault, Sylvain; Chew, Warren; Iera, Silvio; Duncan, Scott Mason; Ren, Jianxin; Assignee Wyeth, John, and Brother Ltd., USA; 2004; Patent Information; Aug 12, 2004; WO 2004066919 A2

Neratinib Maleate - Synthetic Route 9

Neratinib Maleate route09

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Process for preparation of Neratinib and intermediates thereof; Zhang, Rongxia; Liu, Zheng; Zhang, Qiang; Xia, Xiangfei; Wu, Mingjun; Chen, Ji; Chen, Weiming; Li, Jianfeng; Shen, Jingshan; Assignee Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Peop. Rep. China; Topharman Shanghai Co., Ltd.; Topharman Shandong Co., Ltd.; 2012; Patent Information; Oct 17, 2012; CN 102731395 A

Neratinib Maleate - Synthetic Route 10

Neratinib Maleate route010

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Process for the preparation of neratinib maleate; Zhou, Feng; Jin, Hua; Zheng, Yongyong; Huang, Meihua; Meng, Xin; Assignee Shanghai Xunhe Pharmaceutical Technology Co., Ltd., Peop. Rep. China; 2016; Patent Information; Feb 17, 2016; CN 105330646 A