使用聚合物辅助纯化技术进行溶液相化学库合成。

Solution-phase chemical library synthesis using polymer-assisted purification techniques.

作者信息

Parlow J J, Devraj R V, South M S

机构信息

Department of Combinatorial and Parallel Medicinal Chemistry, Searle Discovery Research, Monsanto Co., 800 North Lindbergh Boulevard, Saint Louis, MO 63167, USA.

出版信息

Curr Opin Chem Biol. 1999 Jun;3(3):320-36. doi: 10.1016/S1367-5931(99)80049-0.

DOI:10.1016/S1367-5931(99)80049-0

PMID:10359715

Abstract

During the past few years, polymer-assisted solution-phase synthesis has become a prevalent method for the parallel synthesis of chemical libraries. This methodology allows for intermediate and final product purification by various resin-based sequestration techniques, which allow for the removal of excess reactants, by-products or side products from solution-phase reactions. The methodology has continued to expand, providing the practitioner with a broad range of ingenious purification methods, allowing single-step transformations as well as multistep syntheses to be performed in solution. The polymer-assisted solution-phase technology is currently being utilized for both the synthesis of lead generation and lead optimization libraries in the pharmaceutical arena and has also expanded into other disciplines.

摘要

在过去几年中，聚合物辅助溶液相合成已成为化学文库平行合成的一种普遍方法。该方法允许通过各种基于树脂的分离技术对中间体和最终产物进行纯化，从而能够从溶液相反应中去除过量的反应物、副产物或侧产物。该方法不断扩展，为从业者提供了广泛的巧妙纯化方法，使得单步转化以及多步合成都能在溶液中进行。聚合物辅助溶液相技术目前在制药领域用于先导化合物生成库和先导化合物优化库的合成，并且也已扩展到其他学科。