摘要
中国是癌症大国,而肺癌位居癌症之首。为开发一套工业化可行、生产成本低的肺癌特效药艾维替尼的合成工艺,以2,4-二氯-7H-吡咯并[2,3-d]嘧啶为起始原料,经乙酰化、醚化、Buchwald-Hartwig交叉偶联、硝基还原、脱保护等工序制得液相归一法含量为99.12%的艾维替尼,工艺简单,总收率为80.59%。该合成工艺的突出亮点是使用的溶剂种类少、操作弹性大、工序产品纯化方式简单、原料来源广泛,可为规模化生产提供一定的借鉴。
China is a major cancer country,and lung cancer ranks first in cancer.In order to develop a synthetic process for the commercialization of a lung cancer specific drug Avitinib with industrial feasibility and low production cost,2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine was used as the starting material and acetylated,etherification,Buchwald-Hartwig cross-coupling,nitro reduction,deprotection and other processes to obtain a liquid phase normalization method of Avitinib with a content of 99.12%.The process is simple,the total yield is 80.59%.The outstanding highlights of this synthetic process are the small number of solvents used,the high flexibility of operation,the simple purification of process products,and the wide range of raw material sources,which can provide a certain reference for large-scale production.
作者
林韦康
高奇
江晓明
武立靖
LIN Wei-kang;GAO Qi;JIANG Xiao-ming;WU Li-jing(Zhejiang Yuntao Biotechnology Co.,Ltd.,Shaoxing,Zhejiang 312369,China;Aiyinuo Technology Co.,Ltd.,Zhuji,Zhejiang 311800,China;Nanjing Legend Pharmaceutical&Chemical Co.,Ltd.,Nanjing,Jiangsu 210000,China)
出处
《浙江化工》
CAS
2019年第12期10-16,共7页
Zhejiang Chemical Industry
