1426125-50-9Relevant articles and documents
Evolution of the process for the preparation of a selective erbb vegf receptor inhibitor
Mudryk, Boguslaw,Joshi, Amit,Ortiz, Adrian,Young, Ian S.,Sawyer, James R.,Zheng, Bin,Sugiyama, Masano,Shi, Zhongping,Müslehiddino?lu, Jale,Corbett, R. Michael,Kronenthal, David R.,Conlon, David A.
supporting information, p. 305 - 312 (2013/04/10)
An efficient synthetic route to the potent and selective ErbB VEGF receptor inhibitor, BMS-690514 (1) is described. Strategic modifications in both approach and procedure addressed several issues, which led to a safe, efficient, and economical process for the preparation of multi-kilogram quantities of 1. The convergent route involves alkylation of a suitably protected (3R,4R)-4-aminopiperidin-3-ol with the triethyl(alkyl)ammonium salt of a functionalized pyrrolotriazine 3a followed by deprotection to provide 1 as the crystalline free base. Georg Thieme Verlag Stuttgart - New York.