【摘要】 为使阿西替尼制备工艺适合工业化生产,且生产过程稳定,制备过程安全、绿色环保.以6-溴吲唑和2-巯基-N-甲基苯甲酰胺为起始原料,经过缩合硫醚化、溴化剂NBS溴化吲唑环、烯烃Heck偶联制备阿西替尼.通过实验和放大验证,该路线具有起始原料市场易得,反应条件温和,制备过程对环境污染少,操作过程简易、安全可靠,反应后处理简单,反应总收率高,产品成本相对低廉,相对其他合成路线有更适合工业化生产的明显竞争优势.更多还原

【Abstract】 This paper made axitinib preparation process suitable for industrial production and the production process stable,the preparation process safe and environment friendly. Axitinib was synthesized from 6-bromoindazole condensation with 2-mercapto-N-methyl benzamide,conversion indazole compound with NBS by brominating to bromide,then Bromide by Heck coupling with 2-vinylpyridine get axitinib. Checked by experiments and scale-up,this route has readily available raw materials,mild reaction conditions,less pollution,operation simple and safe and reliable,obvious advantages of easy to deal the experimental post-processing,good total yield. It was more suitable for industrial production that has competitive cheaper cost comparative to other synthetic routes.更多还原