Synthesis of the Degradation Impurity of Rivaroxaban

OBJECTIVE To perform the quality of rivaroxaban which was a kind of anticoagulant drug, three degradation impurities A, B and C were synthesized and characterized. METHODS Rivaroxaban (1 ) was used as starting material to prepare Impurity A , impurity B was synthesized by hydrolyzing impurity A , and impurity C was obtained from impurity A by substitution reaction. RESULTS The structures of the three impurities had been verified by ¹H-NMR and ¹³C-NMR and MS. Their purities were over 99.0% (detected by HPLC). CONCLUSION The synthetic degradation impurities can be used as the reference substance of the impurities in the quality control of rivaroxaban.