Swamy K M K, Yeh Wen-Ben, Lin Mei-Jung, Sun Chung-Ming
Laboratory of Combinatorial Drug Discovery, Department of Chemistry, National Dong Hwa University, Shou-Feng, Hualien 974, Taiwan.
Curr Med Chem. 2003 Nov;10(22):2403-23. doi: 10.2174/0929867033456594.
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 been emerged as a promising tool in generating large numbers of structurally diverse molecules in a manner rapid and parallel. Microwave-assisted solid/liquid phase combinatorial synthetic techniques have been proved efficient in reducing 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.
在药物研发中，先导化合物的识别与优化一直是药物化学家面临的挑战。为满足生物靶点的筛选目的，人们制备了大量从简单到复杂、从小分子到大分子的有机化合物。传统的溶液相合成方法由于反应时间长、后处理繁琐以及纯化问题，难以满足药物研发中对有趣化合物的需求。相比之下，聚合物负载的组合库合成方法作为一种有前景的工具出现了，它能够以快速且平行的方式生成大量结构多样的分子。微波辅助的固/液相组合合成技术已被证明能有效将反应时间从数天、数小时缩短至数分钟、数秒，更有前景的是还能提高产率并获得高纯度产物。本文综述了微波化学技术背后的理论，以及其在聚合物负载组合合成中的应用的最新进展。
