摘要
罗沙司他是一种新型缺氧诱导因子(HIF)脯氨酰羟化酶(PH)抑制剂,临床用于治疗由透析依赖性慢性肾病(DD-CKD)以及非透析依赖性慢性肾病(NDD-CKD)引起的贫血。本文根据起始原料的不同总结了罗沙司他的9条合成路线,并对各条路线进行了评价。其中,构建异喹啉环、C-1位甲基化和C-4位羟基化是合成的关键步骤。
Roxadustat is a novel hypoxia-inducible factor(HIF) prolyl hydroxylase(PH) inhibitor for clinical treatment of anemia caused by dialysis-dependent chronic kidney disease and non-dialysis dependent chronic kidney disease. In this paper, 9 synthetic routes of roxadustat according to different starting materials and intermediates were summarized and evaluated. Among them, the construction of isoquinoline ring, methylation at the C-1 position and hydroxylation at the C-4 position are key steps in the synthetic routes.
作者
张其伟
周嘉第
陈永健
李坚军
ZHANG Qiwei;ZHOU Jiadi;CHEN Yongjian;LI Jianjun(College of Pharmaceutical Sciences,Zhejiang University of Technology,Hangzhou 310014)
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2019年第11期1237-1245,共9页
Chinese Journal of Pharmaceuticals
作者简介
张其伟(1995—),男,硕士研究生,专业方向:药物及中间体的合成。E-mail:869177384@qq.com;通信联系人:李坚军(1977—),男,教授,博士,从事药物及中间体的合成研究。E-mail:lijianjun@zjut.edu.cn。
