529508-57-4Relevant articles and documents
Development of a practical synthesis of a functionalized pyrrolo[2,1-f][1,2,4]triazine nucleus
Zheng, Bin,Conlon, David A.,Corbett, R. Michael,Chau, Melissa,Hsieh, Dau-Ming,Yeboah, Agnes,Hsieh, Daniel,Mueslehiddinoglu, Jale,Gallagher, William P.,Simon, Jeffrey N.,Burt, Justin
, p. 1846 - 1853 (2013/01/15)
Functionalized pyrrolotriazine 1b is a key heterocyclic building block in the synthesis of BMS-690514, a potent anticancer agent. Described herein are our development activities that led to the efficient preparation of 1b on a large scale. The key transformations include a selective C-alkylation of an oxalacetate salt with a hydrazonyl bromide to form a 2-hydrazonoethyl-3- oxosuccinate, followed by cyclodehydration to an aminopyrrole. Subsequent deprotection and condensation with formamidine afforded the pyrrolotriazine scaffold. Further elaboration of this core provided the desired pyrrolotriazinyl amine.
New C-5 substituted pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases
Mastalerz, Harold,Chang, Ming,Chen, Ping,Dextraze, Pierre,Fink, Brian E.,Gavai, Ashvinikumar,Goyal, Bindu,Han, Wen-Ching,Johnson, Walter,Langley, David,Lee, Francis Y.,Marathe, Punit,Mathur, Arvind,Oppenheimer, Simone,Ruediger, Edward,Tarrant, James,Tokarski, John S.,Vite, Gregory D.,Vyas, Dolatrai M.,Wong, Henry,Wong, Tai W.,Zhang, Hongjian,Zhang, Guifen
, p. 2036 - 2042 (2007/10/03)
Novel C-5 substituted pyrrolotriazines were optimized for dual EGFR and HER2 protein tyrosine kinase inhibition. The lead compound exhibited promising oral efficacy in both EGFR and HER2 driven human tumor xenograft models. It is hypothesized that its C-5
SYNTHETIC PROCESS
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Page/Page column 19, (2008/06/13)
The present invention provides a process for preparing compounds of formula (IV), or a pharmaceutically acceptable salt thereof. The compounds prepared by the process of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER