Liu Qing-yong
2007
Citations
0
Influential Citations
0
Citations
Journal
Journal of Chemical Engineering of Chinese Universities
Abstract
As an inhibitor of topoisomerase Ⅰ,the topotecan hydrochloride,a soluble analogue of camptothecin,is broadly used to treat cancer.Here a new procedure for rapid synthesis of topotecan hydrochloride from 10-hydroxycamptothecin via Mannich reaction with the help of ultrasound was presented.The influences of reaction temperature,the frequency of ultrasound used and reaction time on the reaction yield were investigated,and through the single factor tests,the optimum reaction conditions were determined as follows:reaction temperature of 40 ℃,ultrasonic frequency of 40 kHz and reaction time of 120 min.Under above reaction conditions,the average yield of topotecan hydrochloride can reach up to 95.54%,and the obtained compounds were characterized by Fourier transform infrared spectroscopy,mass spectrum and nuclear magnetic resonance.The experimental results show that,compared with the traditionally used Mannich reaction with stirring,the proposed new procedure of using ultrasound is safer and easy to operate,using it not only the reaction time is shortened,but also the reaction efficiency and yield are enhanced.Therefore it is more suitable to be used for industrial production.