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 canc er lines. The process comprises the conversion of starting material, 2-hydroxy- 1,4-naphothoquinone into .beta.-lapachone intermediate, lapachol. The lapach ol 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.