METHOD FOR THE SEPARATION OF PACLITAXEL

摘要

PURPOSE: Paclitaxel is selectively separated from a mixture of the paclitaxel and cephalomannine. CONSTITUTION: A mixture of paclitaxel and cephalomannine is reacted with aliphatic alcohol such as methanol, ethanol, t-butanol, n-butanol, n-propanol and 2-methyl-1-propanol or amine such as ethanolamine or dimethyl amine at -20-40°C in organic solvent such as dichloromethane in the presence of N-halosuccine imide such as N-bromosuccinimide or N-iodosuccinimide. Thus, a mixture of 100 mg of paclitaxel and cephalomannine of formula 2 is reacted with 1 ml of anhydrous ethanol and 1 drop of sulfuric acid at 0°C in 5 ml of dichloromethane in the presence of 50 mg of N-bromosuccinimide to separate 42.5 mg of paclitaxel of formal 1.