Antineoplastic Agents Azacitidine Synthesis Process

The classification and the mechanism of antitumor agents were discussed in this thesis. The synthesis and approchment of a nucleoside antitumor drug,azacitidine,were introduced in detail.The synthetic method of azacitidine was investigated particularly.After investigating a series of synthetic routes of azacitidine,the best one was determined and each step of the synthetic process was optimized for the goal of reducing cost,simplifying operation procedure and improving yield.The key intermediates and target product were confrimed by MS, ~1H-NMR.The synthetic thechology of 1-O-acteyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose,1,2,3,5-tetra -O-acetyl-,β-D-ribose,5-azacytosine and other intermediates were investigated in detail.And the microwave-aid reaction was introduced to shorten reaction time and save solvent dosage.The optimized process has low cost,simplified operation and other advantages which provide avaiable technical support for industrial production.A new procedure was designed for the synthesis of azacitidine independently,and desired product was obtained.This synthetic route has the advantage of fewer steps,convenient operation,but the yield still not satisfied and need to be further optimized.