Improved Manufacturing Process for Pyronaridine Tetraphosphate

Bulletin of the Korean chemical society

Seung Soo Yoon¹  Dong Won Lee¹  Jun Ho Cho¹  Seung Kyu Lee¹ 

关键词: Antimalarial agent;    Pyronaridine tetraphosphate;    Manufacturing process;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

Pyronaridine tetraphosphate (1) is a well-known antimalarial drug. However, it required a carefully optimized production process for the manufacture of pyronaridine tetraphosphate. Each step of its manufacturing process was reinvestigated. For the cyclization of 4-chloro-2-(6-methoxy-pyridin-3-yl-amino)-benzoic acid 6 to 7,10- dichloro-2-methoxybenzo[b]-1,5-naphthyridine 5, an improved process was developed to eliminated critical process impurity (BIA). By the redesign of the formation of triphosphate salt, the purity as API grade was increased. Thus, a robust manufacturing process with an acceptable process performance has been developed to produce high quality pyronaridine tetraphosphate.

【 授权许可】

Unknown