Reader John C
Millennium Pharmaceutical Research and Development Ltd, Granta Park, Great Abington, Cambridge, United Kingdom.
Curr Top Med Chem. 2004;4(7):671-86. doi: 10.2174/1568026043451069.
The implementation of appropriate automation can make a significant improvement in productivity at each stage of the drug discovery process, if it is incorporated into an efficient overall process. Automated chemistry has evolved rapidly from the 'combinatorial' techniques implemented in many industrial laboratories in the early 1990's which focused primarily on the hit discovery phase, and were highly dependent on solid-phase techniques and instrumentation derived from peptide synthesis. Automated tools and strategies have been developed which can impact the hit discovery, hit expansion and lead optimization phases, not only in synthesis, but also in reaction optimization, work-up, and purification of compounds. This article discusses the implementation of some of these techniques, based especially on experiences at Millennium Pharmaceuticals Research and Development Ltd.
如果将适当的自动化技术融入到高效的整体流程中，那么它能够在药物研发过程的每个阶段显著提高生产率。自动化化学技术已经从20世纪90年代初许多工业实验室采用的“组合”技术迅速发展而来，早期的“组合”技术主要集中在活性化合物发现阶段，并且高度依赖于源自肽合成的固相技术和仪器设备。现在已经开发出了一些自动化工具和策略，它们不仅能在合成方面，而且能在反应优化、后处理以及化合物纯化等方面对活性化合物发现、活性化合物扩展和先导化合物优化阶段产生影响。本文将特别基于千年制药研发有限公司的经验，探讨其中一些技术的应用。
