310444-84-9Relevant articles and documents
Commercial synthesis of a pyrrolotriazine-fluoroindole intermediate to brivanib alaninate: Process development directed toward impurity control
Pesti, Jaan A.,LaPorte, Thomas,Thornton, John E.,Spangler, Lori,Buono, Frederic,Crispino, Gerard,Gibson, Frank,Lobben, Paul,Papaioannou, Christos G.
, p. 89 - 102 (2014/05/20)
The development of a practical, commercial process for the preparation of 4-fluoro-2-methyl-indol-5-ol and its subsequent coupling with a pyrrolotriazine to form an advanced intermediate of the oncology therapy brivanib alaninate is described. A key aspect is the multikilogram-scale preparation of the fluoroindole intermediate from trifluoronitrobenzene and the subsequent coupling while achieving impurity minimalization. As brivanib alaninate is a high-dose drug, the synthesis of highquality API with low levels of impurities is critical.