A New Synthetic Procedure For Antineoplastic Agent Combretastatin A-4

Research on the improvement of the total synthesis of an antineoplastic drug Combretastatin A-4(CA-4) was described in the dissertation. Presently cancer is one of the most dangerous diseases. CA-4 is becoming more important as an anticarcer agent. CA-4 was isolated from Combretum caffrum, an African bush willow by Pettit in 1987. As a new potent anticancer agent, CA-4 can inhibit the growth of many tumors and a broader market was prospected. But as the industrial production is concerned, the synthetic methods reported have limitation to some extent. For this purpose, research on the new synthsis procedures has been carried out. 3,4,5-Trimethoxybenzyltriphenylphosphonium bromide and 3-hydroxy-4-methoxy benzaldehyde were dissolved in suitable solvents, such as alcohol, acetonitrile, acetone and heated at reflux under nitrogen protection in the presence of potassium carbonate, sodium carbonate, potassium hydroxide and sodium hydroxide respectively,yielding CA-4. The crude product was transformed into pure cis-CA4 by photochemical method and recrystallization.