Li-Juan Xing
2009
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Journal
Bulletin of the Academy of Military Medical Sciences
Abstract
Objective:To improve the synthetic route and synthesize 4-[(2-methylquinolin-4-yl]methoxy) benzoic acid,which is a key intermediate for the synthesis of β-benzamido TACE inhibitors.Methods:The target compound was synthesized from 2-methylquinoline by hydroxymethylation,chlorination,etherification and hydrolysis.Result and Conclusion:The 1H-NMR and MS data of the intermediates and the target compound were identical with those reported in literature.With this improved route the total yield is 47.5%.This improved synthetic route is convenient,efficient and cost-effective.