Mesozoic magmatites in the Zijinshan region are composed of Late Jurassic granite pluton (157~140 Ma) and Early Cretaceous volcano-intrusive complexes (128~94 Ma), in which the latter is related to large-scale Cu-Au mineralizations of this region. In addition, the Caixi monzogranite with a zircon U-Pb age of 137 Ma was intruded after the granite pluton and before the volcano-intrusive complexes. Geochemistry of major and trace elements for Late Jurassic granites show that they were derived from continental crustal melting under lower pressure during the Indosinian to Early Yanshanian intracontinental orogeny. In comparison with the Late Jurassic granite, the Early Cretaceous volcano-intrusive complexes exhibit elevated Al, Ti, Sr, Cr, Ni, Zr, Cu, Au and Ag value, enrichment of LREE, lack of obviously negative europium anomaly, and lower Sn, W, Rb/Sr and Sr-O isotope ratio values. Their Sr/Y-Y and Ni-Cr relationship coincides with partial melting curves of MORE leaving a 10% garnet amphibolite or eclogite, that shows they were derived from partial melting of oceanic crustal under mantle upwelling and regional extension. Geochemistry of major and trace elements of the Caixi monzogranite lies between the Late Jurassic granite and the Early Cretaceous volcano-intrusive complexes giving a geochemical mark for regional tectonic inversion from compression to extension. Geochemistry of Mesozoic magmatites in the Zijinshan region provides an evidence for that large-scale Cu-Au mineralizations in this region formed under tectonic inversion environment from compression to extension.