Synthesis of Vatalanib

Route1

1. Altmann K.-H., Mett H., Wood J. et all. Phthalazines with angiogenesis inhibiting activity. EP 0970070, WO 9835958

2. DE 1061788; GB 871753



Route2

1.Frei J., Bold, G., Altmann, K.-H.  et al.; New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. J Med Chem 2000, 43, 12, 2310

2.Manly, D.G.; Tilford, C.H.; Richardson, A.; Stock, A.M.; Amstutz, E.D.; A Study of the chemistry of pyrophthalone and related compounds. J Org Chem 1958, 23, 373-80

3.Andersen, L.; Pedersen, E.B.; Synthesis of 4-arylamino-1H-pyrazolo[3,4-d]pyrimidines. Acta Chem Scand Ser b 1988, B42, 492-3