Standardization protocols and optimized precursor sets for the efficient application of automated parallel synthesis to lead optimization: A Mitsunobu example
Standardization protocols and optimized precursor sets for the efficient application of automated parallel synthesis to lead optimization: A Mitsunobu example
复制标题
DOI：
10.1021/cc010090j
复制
发表时间：
2002-09-01
影响因子：
--
通讯作者：
Vasudevan, A
中科院分区：
文献类型：
--
作者：
Gentles, RG;Wodka, D;Vasudevan, A
已经开发了一种策略，用于有效地应用自动化并行合成药物发现中采用的铅优化过程的特定方面。该方法涉及使用一组前体合成化合物集合，这些前体旨在涵盖既定的药物化学原理，并且针对特定的化学转化进行了同步优化。该策略说明使用自动化Mitsunobu协议采用套脂肪醇和酚类作为前体。前者已被格式化为执行简单的烷基同系化练习，后者被设计用于基于多样性的研究。
A strategy has been developed for the efficient application of automated parallel synthesis to specific aspects of the lead optimization processes employed in drug discovery. The method involves the synthesis of collections of compounds using sets of precursors designed to encompass established medicinal chemistry principles and that have been concurrently optimized with respect to a specific chemical transformation. The strategy is illustrated using an automated Mitsunobu protocol employing sets of aliphatic alcohols and phenols as precursors. The former has been formatted to perform simple alkyl homologation exercises, with the latter being designed for use in diversity-based studies.