a novel process for synthesizing β - 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 β - lapachone intermediate , lapachol . the lapachol is then converted to β - lapachone by treatment with sulfuric acid and purified by recrystallization from ethanol . this novel process is extremely simple and provides β - lapachone in excellent quality and high yield .