Design and synthesis of novel 20-substituted hydroxycamptothecin derivatives

Camptothecin (CPT) is a potent antitumor alkaloid isolated in 1966 by M.E. Wall. Clinical use of camptothecin in cancer therapy, however, was limited by its poor water solubility. Recently, there is a growing tendency to develop some new methods for the synthesis of novel derivatives to solve the problem. In this paper, we'd like to report the design and synthesis of a novel series of 20-substituted Hydroxycamptothecin to increase the water solubility. All the five products have never been reported before. All the products and important intermediates were characterized by 1HNMR and LC-MS spectra. ? Springer-Verlag Berlin Heidelberg 2014.