FUMARATE OF PYRROLOPYRIMIDINONE DERIVATIVE AND PROCESS FOR PREPARING IT

摘要

A fumarate of pyrrolopyrimidinone derivative is provided to prevent and treat diseases associated with PDE5(phosphodiesterase 5) by inhibiting the enzyme activity, and improve stability of the compound by inhibiting hygroscopicity and corrosion properties and enhancing stability against heat and light. A PDE5 inhibitor, fumarate of pyrrolopyrimidinone derivative represented by the formula(1) is a crystalline acid addition salt prepared by solubilizing fumaric acid represented by the formula(3) in a solvent selected from water, acetone, methanol, ethanol, isopropanol and acetonitrile, slowly adding pyrrolopyrimidinone derivative represented by the formula(2) into the fumaric acid solution, stirring the mixture at room temperature for 1 hour, removing the solvent through concentration under reduced pressure, filtering the prepared solid, washing the filtered solid with solvent, and drying the washed solid at 50 deg.C under vacuum condition.