磷酸氯喹中有关物质N-氧化氯喹的合成研究

Research on the Synthesis of Chloroquine N-oxide,a Related Substance in Chloroquine Phosphate

研究了磷酸氯喹中有关物质N-氧化氯喹的合成,以磷酸氯喹为原料,利用双氧水做氧化剂进行N-氧化反应制备目标化合物,产物经过质谱和核磁共振波谱进行结构确证,产品为与14和15(15’)号碳相连的N原子被氧化的产物,产品收率88%。进一步对N-氧化氯喹以盐酸、磷酸和硫酸进行酸化制备了其不同的盐,以期望可以得到固体产物,不同的盐仍以液体形式存在。

Chloroquine N-oxide,the related substance of chloroquine phosphate,was synthesized by N-oxidation reaction using hydrogen peroxide and chloroquine phosphate as raw material and was confirmed by MS and NMR.The target product is the oxidation product of N-atom connected with carbon 14 and 15(15')and the yield is 88%.Chloroquine N-oxide was further acidified with hydrochloric acid,phosphoric acid and sulfuric acid to prepare its different salts.