An expeditious synthesis of imatinib and analogues utilising flow chemistry methods

被引：78

作者：

Hopkin, Mark D. ^{[1
]}

Baxendale, Ian R. ^{[2
]}

Ley, Steven V. ^{[1
]}

机构：

[1] Univ Cambridge, Dept Chem, Cambridge CB2 1EW, England

[2] Univ Durham, Dept Chem, Durham DH1 3LE, England

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2013年 / 11卷 / 11期

基金：

英国工程与自然科学研究理事会;

关键词：

RHODIUM-CATALYZED HYDROFORMYLATION; CROSS-COUPLING REACTIONS; ENABLING TECHNOLOGY; AMINATION; EFFICIENT; REACTORS; LIGANDS; AMINES;

D O I：

10.1039/c2ob27002a

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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.

引用

页码：1822 / 1839

页数：18

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