【摘要】 目的:合成非索那定。方法:以苯乙酸乙酯为起始原料,经甲基化、F-C酰化、N-烷基化、还原和水解等反应制得非镇静抗组胺药(NSA)非索那定。结果:N-烷基化反应中改用乙腈为溶剂,提高了溶解性。加快了反应速度,提高了产物的纯度与收率;羰基还原反应由催化加氢改为硼氢化钠还原,方便了操作,便于今后的大批量制备。结论:该方法原料易得、操作简便,总收率40.7％。更多还原

【Abstract】 Objective:To synthesize fexofenadine. Methods: By using ethyl 2-benzeneacetate as starting material, fexofenadine was prepared by a reaction sequence of methylation, F-C acylation, N-alkylation,reduction and hydrolysis. Results:The N-alkylation using MeCN as solvent and the reduction via NaBH4 benefited significantly the purities and yields of the products. Conclusion:The improved synthetic route featured accessible starting materials,easy performance and better total yield (40.7% ).更多还原