APHIDICOLIN DERIVATIVE, SYNTHESIS THEREOF AND CARCINOSTATIC AGENT

摘要

NEW MATERIAL:The aphidicolin derivative of formula I. USE:Useful as a carcinostatic agent applicable by oral or parenteral administration. It is converted to pharmaceutical preparation by using a surfactant, vehicle, lubricant, adjuvant, etc. The ratios of the above components in the preparation are e.g. 0.3-15wt% active component, 85-99.4% vehicle such as lactose, 0-20% lubricant such as magnesium stearate, 0-20% surfactant such as alcohol and 0.3-20% film-forming substance such as cellulose. PREPARATION:The compound of formula I can be produced by reacting the compound of formula II with crotonic anhydride in a solvent such as pyridine in an inert gas stream at room temperature for 12-24hr.