For several decades, interest in the synthesis pyrrole and pyrrolopyrimidine increases due to the importance of these heterocycles both from chemical and biological points of view. They possess several biological activities such as antimicrobial, analgesic, anti-inflammatory, anti-cancer, anti-viral, anti-convulsant, anti-hyperlipidemic, anti-depressant, antidiabetic, anti-allergic activities. These findings motivated us to present this review which highlights different methods of the synthesis of pyrrole and pyrrolopyrimidine derivatives as well as their biological importance from the past to recent years.