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目的 优化催眠药酒石酸唑吡坦的生产工艺.方法 以6-甲基-2-(4-甲基苯基)咪唑[1,2-a]吡啶(2)为原料,经草酰氯酰化、甲醇酯化后得到中间体2-(6-甲基-2-(4-甲基苯基)咪唑[1,2-a]吡啶)-2-氧代乙酸甲酯,经过Wolff-Kishner-黄鸣龙还原得到6-甲基-2-(4-甲基苯基)咪唑并[1,2-a]吡啶-3-乙酸(唑吡坦酸),唑吡坦酸与二甲胺缩合酰化得到N,N,6-三甲基-2-(4-甲基苯基)咪唑并[1,2-a]吡啶-3-乙酰胺(唑吡坦),最后与L-(+)-酒石酸成盐得到酒石酸唑吡坦.结果与结论 优化后的工艺路线比原生产工艺缩短3步反应,总收率为39.0％(以2为原料计),产物纯度高达99.5％.酒石酸唑吡坦的结构经MS、1 H-NMR谱确证,改进后的工艺合成路线原料价廉、易得、低毒,反应条件温和,后处理简单,成本低,适合工业化生产.“,”Zolpidem tartrate,a GABA inhibitor,is used for the treatment of insomnia.An improved synthetic process of zolpidem has been developed in this paper.Zolpidem tartrate was synthesized from 6-methyl-2-(p-tolyl) imidazo [1,2-a]-pyridine via oxalylation and esterification,then subjected to HUANG Ming Long reduction,followed by condensation with dimethylamine and salt formation,the total yield of zolpidem tartrate was 39.0％ (based on 6-methyl-2-(p-tolyl) imidazo [1,2-a]-pyridine).The HPLC purity of the final product is 99.5％.The improved process has many advantages compared with those reported procedures,such as inexpensive materials,low cost,milder reaction conditions,higher yield,for which it's more suitable for industrial production.