HEMITARTRATE OF PYRROLOPYRIMIDINONE DERIVATIVE AND PROCESS FOR PREPARING IT

摘要

A hemitartrate of pyrrolopyrimidinone derivative as a PDE5(phosphodiesterase 5) inhibitor is provided to satisfy physicochemical conditions suitable as a pharmaceutically acceptable salt including low hygroscopicity, suitable solubility, low adhesive properties of tablet, improved stability and convenient mass production. A hemitartrate of pyrrolopyrimidinone derivative represented by the formula(1) is prepared by preparing tartaric acid-containing reaction solution by solubilizing 0.5-20 wt.% of tartaric acid in water or organic solvent, mixing the tartaric acid-containing reaction solution with SK-3530 free base represented by the formula(3) as pyrrolopyrimidinone derivative, mixing and reacting the mixture to obtain a solid, and filtering, washing and drying the solid at -30 to 50 deg.C. A pharmaceutical formulation for preventing and treating diseases associated with PDE5 comprises the hemitartrate of pyrrolopyrimidinone derivative represented by the formula(1), wherein the daily dosage of hemitartrate of pyrrolopyrimidinone derivative is 10.0-200.0 mg/kg.