Combinatorial Synthesis of Small Molecule Libraries by Microwave Technology
Pp. 485-510 (26)
Lead identification and optimization is always a challenge to the medicinal chemists in drug discovery. Numbers of simple to complex and smaller to bigger organic compounds are prepared to meet the screening purpose of biological targets. Conventional solution phase synthetic methodologies are lacking the speed to run along with the need of medicinally interesting compounds due to their long reaction time, tedious work-up and purification problems. Alternatively opted polymer-supported synthesis of combinatorial libraries has emerged as a promising tool in generating large numbers of structurally diverse molecules parallelly and rapidly. Microwave-assisted solid/liquid phase combinatorial synthetic techniques have proved their efficiencies to reduce the reaction time from days & hours to minutes & seconds and more promisingly to produce improved yields with high purities. This review briefs about the theory behind microwave chemical technology and glimpses of recent advancements in its application on polymer supported combinatorial synthesis.
Laboratory of Combinatorial Drug Discovery, National Dong Hwa University, Shou-Feng, Hualien 974, Taiwan.