700-37-8Relevant articles and documents
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro- N 2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)- N 4-(2-(isopropylsulfonyl) phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials
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
, p. 5675 - 5690 (2013/08/23)
The synthesis, preclinical profile, and in vivo efficacy in rat xenograft models of the novel and selective anaplastic lymphoma kinase inhibitor 15b (LDK378) are described. In this initial report, preliminary structure-activity relationships (SARs) are described as well as the rational design strategy employed to overcome the development deficiencies of the first generation ALK inhibitor 4 (TAE684). Compound 15b is currently in phase 1 and phase 2 clinical trials with substantial antitumor activity being observed in ALK-positive cancer patients.
Tetramethylammonium chloride as a selective and robust phase transfer catalyst in a solid-liquid halex reaction: The role of water
Sasson, Yoel,Negussie, Samuel,Royz, Michael,Mushkin, Noam
, p. 297 - 298 (2007/10/03)
Tetramethylammonium chloride (TMAC) is an effective phase transfer catalyst for the selective chloride/fluoride exchange reaction of activated aryl chlorides with potassium fluoride provided that the amount of water in the system is limited and controlled.