聚合物固载试剂在手性药物合成中应用的研究进展.pdf

• 338 • 现代药物与临床 Drugs Clinic 第 27 卷 第 4 期 2012 年 7 月 聚合物固载试剂在手性药物合成中应用的研究进展 1,2 1* 1* 1 1,2 张伟光 ，蔡志强 ，徐为人 ，汤立达 ，刘洪强 1. 天津药物研究院 释药技术与药代动力学国家重点实验室 天津市新药设计与发现重点实验室，天津 300193 2. 天津中医药大学，天津 300193 摘 要：当前手性药物合成的研究已成为国际药学研究领域的热点之一，近几年发展起来的在聚合物固载试剂条件下进行的 不对称合成由于其各种优点，引起了药学界广泛的关注。无论从经济角度还是从“绿色化学”角度考虑，聚合物固载试剂的 巨大潜力势必会推动手性药物合成技术的迅速发展。从抗肿瘤类、抗生素类、天然产物类和生物化学类活性物质对近几年来 聚合物固载试剂在手性药物合成方面的应用进行简述，并对其前景进行展望。 关键词：手性药物；聚合物固载；生物活性；天然产物；绿色化学 中图分类号：R91 文献标志码：A 文章编号：1674 - 5515(2012)04 - 0338 - 09 Advances in studies on application of polymer-supported reagents in synthesis of chiral drugs 1, 2 1 1 1 1, 2 ZHANG Wei-guang , CAI Zhi-qiang , XU Wei-ren , TANG Li-da , LIU Hong-qiang 1. State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Key Laboratory of Molecular Design and Drug Discovery, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China 2. Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China Abstract: Currently, the synthesis of chiral drugs has become one of the pharmaceutical hot researches in the world. Using polymer-supported reagents to develop asymmetric synthesis of chiral drugs with various advantages has aroused widespread concern in the field of pharmacy. The great potential of polymer-supported reagents will certainly promote the synthesis technology of chiral drugs to rapid development both from the view of economic and the consideration of “green chemistry”. In the paper, application of polymer-supported reagents in synthesis of chiral drugs from antitumor agents, antibiotics, natural products, and biochemical substances aspects is reviewed and the prospects are looked forward. Key words: chiral drug; polymer-supported; biological activity; natural p