Abstract: The objective of this investigation was to synthesize and characterize some substitutive derivatives of Tranexamic Acid (TA) and their copper (II) complexes. N-Phthaloyltranexamic Acid (A-1), N-Acetyltranexamic Acid (A-2), Di-Tranexamate Diaquo Copper (II) (C-1), Di-N-Phthaloyltranexamate Diaquo Copper (II) (C-2) and Di-N-Acetyltranexamate Diaquo Copper (II) (C-3) were synthesized, using novel and reproducible procedures. These compounds were characterized by exploiting the techniques such as Fourier Transform Infra Red (FTIR) Spectroscopy, Mass Spectroscopy (MS) and FT 1H NMR. Different methods, reported in the literature, have successfully been applied for qualitative and structural characterization of these compounds. C-1 showed unidentate bonding of carboxylic group to copper (II) while C-2 and C-3 indicated bidentate bonding of carboxylate group to copper (II).