Abstract A simple, facile, and convenient route is adopted for the synthesis of 4,9-dimethoxynaphthalide (4,9-DMN); an analog of naturally occurring naphthalene lactone family. It is achieved without involving a tedious and hazardous lithiation step using 3-(bromomethyl)-1,4-dimethoxy-2-naphthaldehyde as key intermediate through base catalyzed oxidative cyclization resulting in a five-membered lactone ring. This compound exhibits significant anti-fungal activity against Candida albicans while it is found to be less toxic towards MCF-7 cancer cell line with IC50 value less than 250 µM. Graphical Abstract

中文翻译：

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一种简便合成生物活性 4, 9-二甲氧基萘的非锂化途径

摘要 采用一条简单、简便、方便的路线合成4,9-二甲氧基萘(4,9-DMN)；一种天然存在的萘内酯家族的类似物。它的实现不涉及使用 3-(溴甲基)-1,4-二甲氧基-2-萘醛作为关键中间体通过碱催化氧化环化产生五元内酯环的繁琐和危险的锂化步骤。该化合物对白色念珠菌表现出显着的抗真菌活性，同时发现它对 MCF-7 癌细胞系的毒性较小，IC50 值小于 250 µM。图形概要