Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands
Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands
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DOI：
10.1016/s0960-894x(00)00104-9
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发表时间：
2000-05-15
影响因子：
2.7
通讯作者：
Terstappen, G
中科院分区：
文献类型：
--
作者：
Rabinowitz, M;Seneci, P;Terstappen, G
以GPI 1046为基础，发展了一种新的固相/液相合成神经亲免素配体的方法。该合成采用固相酯化策略，然后是溶液相的异丙酰胺形成，以产生用于测定的多毫克量的离散化合物。该协议被应用于880个离散化合物的生产库。该策略的一个亮点是使用为高通量开发的新型液体/冰萃取系统对最终化合物进行水萃取纯化。(C)2000年由Elsevier Science Ltd.出版
A novel solid-phase/solution-phase strategy for the synthesis of neuroimmunophilin ligands based on GPI 1046 was developed. The synthesis employs a solid-phase esterification strategy followed by a solution-phase pyruvic amide formation to produce multi-milligram quantities of discrete compounds for assay. The protocol was applied to a production library of 880 discrete compounds. A highlight of the strategy is an aqueous extractive purification of the final compounds using a novel liquid/ice extraction system developed for high throughput. (C) 2000 Published by Elsevier Science Ltd.