Ceritinib

CAT#: H205511

CAS#: 1032900-25-6

Description: Ceritinib, also known as LDK378, is a selective inhibitor of ALK1, a target found in metastatic non-small cell lung cancer (NSCLC). In Phase I trials, LDK378 showed a marked clinical response in 78 patients with anaplastic lymphoma kinase positive (ALK+) metastatic non-small cell lung cancer (NSCLC) who had progressed during or after crizotinib therapy or had not been previously treated with crizotinib. LDK378 blocks the ALK protein and stops it sending growth signals to cancer cells, which may stop them growing. Ceritinib was approved in April 2014.

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Synthetic Routes

Ceritinib - Synthetic Route 1

Ceritinib route01

Synthetic reference

Marsilje, Thomas H.; Pei, Wei; Chen, Bei; Lu, Wenshuo; Uno, Tetsuo; Jin, Yunho; Jiang, Tao; Kim, Sungjoon; Li, Nanxin; Warmuth, Markus; Sarkisova, Yelena; Sun, Frank; Steffy, Auzon; Pferdekamper, AnneMarie C.; Li, Allen G.; Joseph, Sean B.; Kim, Young; Liu, Bo; Tuntland, Tove; Cui, Xiaoming; Gray, Nathanael S.; Steensma, Ruo; Wan, Yongqin; Jiang, Jiqing; Chopiuk, Greg; Li, Jie; Gordon, W. Perry; Richmond, Wendy; Johnson, Kevin; Chang, Jonathan; Groessl, Todd; He, You-Qun; Phimister, Andrew; Aycinena, Alex; Lee, Christian C.; Bursulaya, Badry; Karanewsky, Donald S.; Seidel, H. Martin; Harris, Jennifer L.; Michellys, Pierre-Yves. Synthesis, Structure-Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials. Journal of Medicinal Chemistry. Volume 56. Issue 14. Pages 5675-5690. Journal; Online Computer File. (2013).

Ceritinib - Synthetic Route 2

Ceritinib route02

Synthetic reference

Rao, R. V. Ramana; Oruganti, Srinivas; Ganorkar, Rakesh; Dahanukar, Vilas Hareshwar. Process for preparation of ceritinib. Assignee Dr. Reddy's Laboratories Limited, India. IN 2015CH02858. (2016).

Ceritinib - Synthetic Route 3

Ceritinib route03

Synthetic reference

Murki, Veerender; Vasam, Sridhar; Komati, Shravan Kumar; Gunda, Nageshwar; Badisa, Venkata Rao; Rao, R. V. Ramana; Oruganti, Srinivas; Ganorkar, Rakesh; Dahanukar, Vilas Hareshwar; Katkam, Srinivas; Thatipalli, Poornachander. Process for preparation of ceritinib. Assignee Dr. Reddy's Laboratories Limited, India. WO 2016199020. (2016).

Ceritinib - Synthetic Route 4

Ceritinib route04

Synthetic reference

Yu, Libing; Guo, Maojun; Yang, Qingang; Liu, Huixin. A process for preparing ceritinib and its intermediates. Assignee Alputon Inc., Peop. Rep. China; Shanghai Acebright Pharmaceuticals Group Co., Ltd. CN 105646333. (2016).

Ceritinib - Synthetic Route 5

Ceritinib route05

Synthetic reference

Wu, Xueping; Han, Dong; Shi, Zhuyong. Preparation of Ceritinib. Assignee Nanjing CHICO Pharmaceutical Co., Ltd., Peop. Rep. China. CN 104356112. (2015).