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.