Lapatinib

CAT#: H100490A

CAS#: 231277-92-2

Description: Lapatinib is a synthetic, orally-active quinazoline with potential antineoplastic activity. Lapatinib reversibly blocks phosphorylation of the epidermal growth factor receptor (EGFR), ErbB2, and the Erk-1 and-2 and AKT kinases; it also inhibits cyclin D protein levels in human tumor cell lines and xenografts. EGFR and ErbB2 have been implicated in the growth of various tumor types.

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Synthetic Routes

Lapatinib - Synthetic Route 1

Lapatinib route01

Synthetic reference

Zhang, Yaling; Zhang, Ying; Liu, Juan; Chen, Li; Zhao, Lijun; Li, Baolin; Wang, Wei. Synthesis and in vitro biological evaluation of novel quinazoline derivatives. Bioorganic & Medicinal Chemistry Letters. Volume 27. Issue 7. Pages 1584-1587. 2017

Lapatinib - Synthetic Route 2

Lapatinib route02

Synthetic reference

Petrov, Kimberly G.; Zhang, Yue-Mei; Carter, Malcolm; Cockerill, G. Stuart; Dickerson, Scott; Gauthier, Cassandra A.; Guo, Yu; Mook, Robert A.; Rusnak, David W.; Walker, Ann L.; Wood, Edgar R.; Lackey, Karen E. Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series. Bioorganic & Medicinal Chemistry Letters. Volume 16. Issue 17. Pages 4686-4691. 2006.

Lapatinib - Synthetic Route 3

Lapatinib route03

Synthetic reference

Lackey, Karen Elizabeth; Spector, Neil; Wood, Edgar Raymond, III; Xia, Wenle. 4-Quinazolineamine derivative combination with other antineoplastic agent for cancer treatment, and compound preparation. Assignee Glaxo Group Limited, UK. WO 2002056912. (2002).

Lapatinib - Synthetic Route 4

Lapatinib route04

Synthetic reference

Jyothi Prasad, Ramanadham; Adibhatla Kali Satya, Bhujanga Rao; Venkaiah Chowdary, Nannapaneni. A novel process for the preparation of lapatinib and its pharmaceutically acceptable salts. Assignee Natco Pharma Limited, India. WO 2010061400. (2010).

Lapatinib - Synthetic Route 5

Lapatinib route05

Synthetic reference

Li, Hanpu; Li, Jianzhi; Liu, Hai; Chi, Wangzhou; Zhai, Zhijun; Li, Jianxun. Preparation of Lapatinib drug for treating breast cancer. Assignee Shanghai Tianci Biological Valley Engineering Co., Ltd., Peop. Rep. China. CN 106632276. (2017).

Lapatinib - Synthetic Route 6

Lapatinib route06

Synthetic reference

Ma, Wenli; Liu, Hang; Liang, Jianlin. Method for synthesizing lapatinib or its intermediate. Assignee Chengdu Meiruike Biotechnology Co., Ltd., Peop. Rep. China. CN 106432206. (2017).

Lapatinib - Synthetic Route 7

Lapatinib route07

Synthetic reference

Ji, Xing; Wang, Wuwei; Xu, Guanhong; Li, Fei; Yao, Shechun. Synthesis of lapatinib. Zhongguo Yiyao Gongye Zazhi. Volume 40. Issue 11. Pages 801-804. 2009.

Lapatinib - Synthetic Route 8

Lapatinib route08

Synthetic reference

Hong, Hao; Gage, James; Lu, Jiangping; Li, Jiuyuan; Shen, Litao; Zhu, Zili; Wang, Zedong. Preparation method of substituted o-aminocyanobenzene, and application for synthesis of Lapatinib. Assignee Asymchem Laboratories (Tianjin) Co., Ltd., Peop. Rep. China; Asymchem Life Science (Tianjin) Co., Ltd.; Tianjin Asymchem Pharmaceutical Co., Ltd.; Asymchem Laboratories (Fuxin) Co., Ltd.; Asymchem Laboratories (Jilin) Co., Ltd. CN 105646405. (2016).

Lapatinib - Synthetic Route 9

Lapatinib route09

Synthetic reference

Yuan, Jianyong; Guo, Qing; Li, Yanwu. A process for preparing lapatinib and its intermediates. Assignee Chongqing University of Medical Sciences, Peop. Rep. China. CN 105085496. (2015).

Lapatinib - Synthetic Route 10

Lapatinib route010

Synthetic reference

Reddy, Muddasani Pulla; Rao, Talasila Sambasiva; Reddy, Satti Venkata; Chowdary, Nekkanti Satish; Chowdhary, Nannapaneni Venkaiah. Process for the preparation of lapatinib. Assignee Natco Pharma Limited, India. IN 2013CH01542. (2014).