齐多夫定生产中叠氮化工艺优化

Zidovudine Azide in Production Process Optimization

齐多夫定是重要的抗艾滋病毒药物,也是目前抗艾滋病药物中最基本的组合成分。现有合成方法存在原料来源及成本等问题,研究及改进其合成中的工艺具有重要的经济效益和社会效益。本文分析齐多夫定氧桥工艺的优化到叠氮化物结晶工艺的优化。用车间叠氮甲苯液拉干后得到齐多夫定叠氮化物结晶固体,最终异丙醇和丙酮的方案得到的产品纯度高,溶残合格,但产率较低,耗时太长;甲醇和水的方案得到的产品纯度达97.1%,粗品有45.2 g,但是最后的溶残中甲苯含量过高,不适用于生产;而异丙醇和甲醇方案得到的产品产率较高,溶残合格,但纯度较低。

Zidovudine is important anti-hiv drugs, is currently the most basic composition of anti-aids drugs. The existing problems and the cost of raw material source synthesis method, research and improve its synthesis process has important economic and social benefits. This article from the zidovudine oxygen bridge process optimization to azide crystallization process optimization in his writing. With workshop azide toluene liquid, dry after get zidovudine azide crystalline solid, isopropyl alcohol and acetone solution to get the final product high purity, but the yield is low, dissolve the residual qualified, but time is too long; Methanol and water solution to get the product purity was 97.1%, and the crude product is 45.2 g, but the final solution of residual toluene content is too high, do not apply to the production. And isopropyl alcohol and methanol solution of product yield is higher, but lower purity, finally.