Development and scale-up of an optimized route to the ALK inhibitor CEP-28122

…, RC Roemmele, JJ Haley Jr, DR Mowrey…

Index: Allwein, Shawn P.; Roemmele, Renee C.; Haley, James J.; Mowrey, Dale R.; Petrillo, Daniel E.; Reif, James J.; Gingrich, Diane E.; Bakale, Roger P. Organic Process Research and Development, 2012 , vol. 16, # 1 p. 148 - 155

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Citation Number: 18

Abstract

Evolution of the process strategies to prepare CEP-28122, an anaplastic lymphoma kinase (ALK) inhibitor, is presented. The initial medicinal chemistry route, used for the preparation of key supplies for biological screening, is reviewed. In addition, the process research and development of the final optimized process for manufacture of preclinical and clinical supplies is discussed. Details regarding a blocking group strategy for selective nitration; ...