非索那定的合成  

Synthesis of fexofenadine

作　　者：葛宗明[1] 许学农[1] 李锐[1] 胡跃飞[1] 

机构地区：[1]清华大学化学系,北京100084

出　　处：《中国新药杂志》2004年第2期139-141,共3页Chinese Journal of New Drugs

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％。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% ).

关 键 词：非索那定 组胺H1受体拮抗剂 合成 

分 类 号：R914.5[医药卫生—药物化学] R976[医药卫生—药学]