SYNTHESIS OF BETA-LAPACHONE AND ITS INTERMEDIATES

摘要

A novel process for synthesizing beta -lapachone (beta-lapachone), an agent that has demonstrated significant antineoplastic activity against human cancer lines. The process comprises the conversion of starting material, 2-hydroxy-1,4-naphothoquinone into beta -lapachone intermediate, lapachol. The lapachol is then converted to beta -lapachone by treatment with sulfuric acid and purified by recrystallization from ethanol. This novel process is extremely simple and provides beta -lapachone in excellent quality and high yield.