Synthesis Of Purine Derivatives

Purine derivative is an important pharmaceutical intermediate of extensive funtion. The derivative of adding substitution groups in purine ring s 2 or 6 or 8 atoms are important organism medicine activating substances useful as an antiviral, anticancer, and hypotensor drugs. So study of purine derivative has important meaning.Guanine is acetylated with acetic anhydride in acetic acid to give N²,9-diacetyl--guanine. The optinized factors: reaction temperature is 135℃, V(acetic acid): V(acetic anhydride)=2:1, reaction time is 7.5h. The ratio of yield can be reached 95%. Then N²,9-diacetylguanine of adding phase transfer catalysis TEMAC was chlorized, hydrolysed to give 2-amino-6-chloropurine. The optinized factors: reaction time is 6h, n(N²,9-diacetylguanine):n(POCl₃) =1:3.5, reaction temperature is 80℃. The ratio of yield can be reached 85%. At last, 2-amino-6-chloropurine was iodizated to give 2-amino--6-iodopurine. The optinized factors:n(2-amino-6-chloropurine):n(iodizating agent) = 1:6, reaction time is 2h, reaction temperature is 35°C. The ratio of yield can be reached 93.5%.