利用流动化学方法快速合成伊马替尼及其类似物。
An expeditious synthesis of imatinib and analogues utilising flow chemistry methods.
机构信息
Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, UK.
出版信息
Org Biomol Chem. 2013 Mar 21;11(11):1822-39. doi: 10.1039/c2ob27002a. Epub 2012 Dec 18.
PMID:23247615
Abstract
A flow-based route to imatinib, the API of Gleevec, was developed and the general procedure then used to generate a number of analogues which were screened for biological activity against Abl1. The flow synthesis required minimal manual intervention and was achieved despite the poor solubility of many of the reaction components.
摘要
开发了一种基于流动的路线来制备格列卫的原料药伊马替尼，并利用该通用方法生成了一系列类似物，然后对这些类似物进行了针对 Abl1 的生物活性筛选。尽管许多反应成分的溶解度很差，但该流动合成所需的人工干预最小，并得以实现。
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