Synthesis And Characterization Of Nitrogen Mustards Modified By Schiff Base

Nitrogen mustards are a sort of common chemotherapetic agents. They are no structural specificity and have strong killing effect to various tumor cells. So far, a variety of nitrogen mustard derivatives have been widely used in clinical therapy, but as a type of alkylating agent, nitrogen mustard derivatives also contain their defects. When it inhibit and poison cancer cells, the other active normal cells may be also killed, so lots of side effects can be caused. The other, nitrogen mustards have immunosuppression effect, it can decrease our body's defense function and various infections can be caused by bacteria and virus. So now, how to modify nitrogen mustards'structures and decrease their side effects turn to be a research hotspot. Schiff base has been proved to have bactericidal activity and antivirus effect, especially in recent years, people found schiff base have antitumor activity. To get new antitumor drugs which have lower side effects and higher therapeutic index, this research synthesized 14 nitrogen mustards modified by Schiff base. The contents are as follows:1. Based on largely amount literatures, this paper separately expounded the research and application of chemotherapetic agents, nitrogen mustards and shiff bases.2. Prepared 14 novel nitrogen mustards modified by schiff bases via conventional heating method.3. Also prepared the 14 nitrogen mustards under microwave irradiation, and the two synthesis methods, conventional heating and microwave irradiation were compared, it's showed that preparing schiff bases under microwave irradiation is an efficient method. The reaction condition was also studied and optimized.4. Studied the relationship between the structures of target compounds and the reacton times and yields. The result showed that these compounds' yields increase as the electronegativity of aromatic amines increase, decrease as the steric hindrance of aromatic amines increase; and their reaction time increase as the electronegativity of aromatic amines increase, decrease as the steric hindrance of aromatic amines decrease.5. All of the compound's structures have been characterized by 1H NMR, IR, MS and elemental analysis.