Qian Shan
2010
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Journal
Chinese Journal of Medicinal Chemistry
Abstract
Aim To improve the synthetic procedure of ivabradine.Methods 3,4-Dimethoxybenzaldehyde was used as the starting material to give(1S)-4,5-dimethoxyl-1-(methylaminomethyl)benzocyclobutane(11) by bromination,condensation,reduction,decarboxylation,cyclization,hydrogenation,resolution,hydrolysis,ethyl chlorformate protection and reduction.Then the target compound was obtained by the condensation of 11 and 12.Results and conclusion The structure of the target compound was confirmed by 1H-NMR,MS.The proportion of the ingredients and the method of the postprocessing had been improved in the process of synthesis of the target compound.The improved syntheic way is convenient and might be applied to the industrial manufacture with the increased overall yield from 7.8% to 12.9%.