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One of the main aims of drug discovery process is to generate novel therapeutic agents against the vast number of potential drug targets and this demands the acceleration of the drug discovery process. It is important to look not only at the staggering cost of discovering a new drug but also at the development time. Microwave assisted organic synthesis enhances the drug discovery process by increase in synthetic yields, consistently shorter reaction time and single step synthesis of many conventional multi-step synthetic procedures. In the present article, an attempt has been made to outline the importance of microwave assisted organic synthesis in drug discovery process.