相转移催化合成盐酸萘替芬

以萘和苯乙烯为起始原料 ,在多聚甲醛、冰醋酸和磷酸存在下进行氯甲基化反应 ,制备 1 -氯甲基萘 ,与 3 0 % (质量分数 )甲胺反应得 N-甲基 -1 -萘甲基胺 ;然后苯乙烯与甲醛和盐酸反应生成3 -氯 -苯丙烯 ;再经 N-烃基化反应合成抗真菌药物萘替芬。 N-烃基化反应中用 PEG-40 0 ,PEG-60 0作为固 -液体系相转移催化剂。避免使用昂贵的四氢硼钠 ,合成路线缩短 ,反应条件温和 ,操作简便。作为相转移催化剂的聚乙二醇催化效果优于溴化四丁基胺 ,合成 N-甲基 -1 -萘甲基胺时 ,用 PEG-40 0收率较高 ,合成萘替芬时 ,用 PEG-60 0 ,收率达 90 .6%。

Synthesis of Naftifine by Phase-transfer Catalysis

The naftifine of antifungal pharmaceuticals was synthetized using naphthalene and styrene as raw materials. 1 Chloro methyl naphthalene was made from poly formaldehyde and acetic acid via chloromethy lation. N methyl methylnaphthylamine was made from methylamine. Then, 3 chloro β methylstyrene was produced reacting to styrene and formaldehyde with hydrochloric acid. PEG 400 and PEG 600 worked as phase transfer catalyst in solid liquid phase N alkylation reactions. The route the of synthesis was shortened, and the reacting conditions were moderate. The operating procedure was simple and the raw materials were easy to be acquired. The N alkylation yield was 90.6%.