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Part-IIImpact of Microwave…2. Impact of Microwave Assisted Heating on the Combinatorial and ParallelSyntheses of Compound Libraries for New Drug Discovery Research: A Review2.1 IntroductionMedicinal chemistry has benefited tremendously from the technological advances in thefield of combinatorial chemistry and high-throughput parallel synthesis. Developments ofmethods and technologies have helped accelerate the design, synthesis, purification, andanalysis of compound libraries. These new tools have had a significant impact on bothlead identification and lead optimization in New Drug Discovery Research (NDDR).Large compound libraries can now be designed and synthesized in very short time toprovide valuable leads for new therapeutic targets. 1 Once a chemist has developed asuitable high-speed synthesis of a lead, it is now possible to synthesize and purifyhundreds of molecules in parallel to discover new leads and/or to derive structure–activityrelationships (SAR) in unprecedented timeframes.Microwave-assisted heating under controlled conditions has been shown to be aninvaluable technology for medicinal chemistry and drug discovery applications since itoften dramatically reduces reaction times, typically from days or hours to minutes or evenseconds. Compound libraries can then be rapidly synthesized in either a parallel orsequential (automated) format using this new, enabling technology.Microwave synthesis has the potential to influence medicinal chemistry efforts in at leastthree major phases of NDDR1. Generation of a discovery library;2. Hit-to-lead efforts and3. Lead optimization.A common theme throughout this drug discovery and development process is speed. Tothe pharmaceutical industry and the medicinal chemist, time truly does equal money, andmicrowave chemistry has become a central tool in this fast-paced, time-sensitive field.The short reaction times required by microwave synthesis make it ideal for rapid reactionscouting and optimization, allowing rapid synthesis of large number of NCE’s. 1,2272