Porco J A, Deegan T, Devonport W, Gooding O W, Heisler K, Labadie J W, Newcomb B, Nguyen C, van Eikeren P, Wong J, Wright P
Argonaut Technologies Inc., San Carlos, CA 94070, USA.
Mol Divers. 1997;2(4):197-206. doi: 10.1007/BF01715635.
Solid-phase organic synthesis is now a prevalent activity in drug discovery. In keeping with this keen interest is the need to develop reliable automated synthesis instrumentation as well as polymeric supports and linkers suitable for the full range of organic synthesis applications. In this paper, we review our activities in the development of new and enabling tools for automated chemical synthesis, including the following: (i) new solid supports such as ArgoGel (PS-PEG-based) and Argo-X203 (PS-based); and (ii) the Nautilus 2400 system, a fully closed and inert automated chemistry development workstation. Selected chemistry optimization and synthesis examples performed on the Nautilus and new solid supports will be described.
固相有机合成如今在药物研发中是一项普遍的活动。与这种浓厚兴趣相契合的是,需要开发可靠的自动化合成仪器以及适用于全范围有机合成应用的聚合物载体和连接体。在本文中,我们回顾了我们在开发用于自动化化学合成的新型且实用工具方面所开展的工作,包括以下内容:(i)新型固相载体,如ArgoGel(基于聚苯乙烯 - 聚乙二醇)和Argo - X203(基于聚苯乙烯);以及(ii)Nautilus 2400系统,这是一个完全封闭且惰性的自动化化学开发工作站。将描述在Nautilus和新型固相载体上进行的选定化学优化和合成实例。