Zhuang Wei, Zhao Haiyong, Sun Xiao-qiang
2010
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Chemical Reagents
Abstract
The process for synthesis of 4-(1-(tert-butoxycarbonyl)piperidin-4-ylmethoxy)-3-methoxy-benzoate,a crucial intermediate of vandetanib,was studied.4-piperidinecarboxylate used as the raw material was protected by di-tert-butyl dicarbonate,and then was reduced by LiAlH4 to give N-boc-4-hydroxymethylpiperidine with the intermediate reacting with toluene sulphonyl chloride.Finally the substitution reaction was performed with methyl 4-hydroxy-3-methoxybenzoate to give the title compound.The synthesis process was optimized and the preferred conditions were identified.The total yield of the product was 70.6%.The melting point of the title compound was the same as that reported in the literature,and its structure was confirmed by 1HNMR spectroscopy.