摘要
托匹司他是一种黄嘌呤氧化还原酶(ROX)抑制剂,对痛风有显著的治疗作用,其耐受性好,不良反应小,是目前治疗痛风最有效的药物之一。托匹司他由三唑环片段和两个吡啶环片段拼合而成,其合成关键步骤在于吡啶2-位氰基的引入(Ⅰ)、两个吡啶环的拼接(Ⅱ)和三唑环的构建(Ⅲ)。该文根据各关键步骤的顺序不同,将托匹司他的合成策略分为"Ⅰ+Ⅱ+Ⅲ"、"Ⅱ+Ⅲ+Ⅰ"和"Ⅱ+Ⅰ+Ⅲ"三种策略,并以这3种策略为主线综述了托匹司他自2002年发现至今的合成研究进展。
Topiroxostat,a xanthine oxidoreductase(ROX)inhibitor,has significant therapeutic effects on gout,good tolerance and low incidence of adverse reactions,therefore,is used clinically as one of the most effective drugs for the treatment of gout.Structurally,Topiroxostat was constructed by linking three structural fragments:triazole ring and two pyridine rings.The key synthetic steps include the introduction of pyridine-2-cyano group(Ⅰ),the splicing of two pyridine rings(Ⅱ)and the construction of triazole ring(Ⅲ).Based on the different sequences of the key steps,the synthetic strategies of Topiroxostat fall into three categories:Ⅰ+Ⅱ+Ⅲ,Ⅱ+Ⅲ+Ⅰ,Ⅱ+Ⅰ+Ⅲ.In this paper,the progress in the synthesis of Topiroxostat since its discovery in 2002 has been reviewed.
作者
卢文龙
陈炯
古双喜
徐志强
LU Wen-long;CHEN Jiong;GU Shuang-xi;XU Zhi-qiang(Key Laboratory for Green Chemical Process of Ministry of Education,School of Chemical Engineering&Pharmacy,Wuhan Institute of Technology,Wuhan 430205,China)
出处
《合成化学》
CAS
北大核心
2020年第4期360-370,共11页
Chinese Journal of Synthetic Chemistry
基金
国家自然科学基金面上项目(21877087)
武汉市国际科技合作项目(2017030209020257)。
