Aniline Phthalazine Compounds Design And Synthesis Of Research

In this thesis, we have designed and synthesized VEGF receptor kinase inhibitors . anilinophthazine derivatives.In this paper, the action mechanism and the development of angiogenesis inhibitors were introduced briefly, the inhibitors of VEGF receptor tyrosine kinase were described in detail and the design and synthesis of anilnophthazine derivatives were studied particularly.With PTK787 as the leading compound, some modifications were made at the 1 and 4 positions preserving the phthalazine ring . With phthalic anhydride and malonate as starting materials, a synthetic route was got through and twenty-three target compounds were obtained by addition, bromination, substitution, cyclization, chloro-substituted reaction, amine- substituted reaction, sulfoxide reaction or sulfone reaction ect totally seven to eight steps reactions, which have not been reported in the literatures. The structures of those compounds were confirmed by ~1H-NMR, MS and IR.