Synthesis And Antitumor Activity Of 2-Cyanotetrahvdropyrimidines/Imid-Azoles And Cvanoaryl Substituted Enamine Esters

N-containing heterocycles are a class of organic compounds with significant application value,which widely exist in lots of natural products.Because of their good biological activity,unique chemical modifiability and low toxicity,they are widely used in organic chemistry and other fields.Cyanide compounds have attracted much attention due to their potential physiological activities and medicinal value.On the one hand,cyano compounds are a kind of important nitrogenous compounds,which can be used as important blocks for drug molecular synthesis;on the other hand,cyano compounds have better physiological activities because of their special properties.Based on this,we have designed and synthesized two kinds of cyano heterocyclic compounds.In Chapter 1,the research progress of N-containing heterocycles and cyano compounds,and the research progress of two kinds of important synthons are briefly reviewedIn Chapter 2,a one-step method for the synthesis of 2-cyanopyrimidine/imidazole derivatives from N-benzylnitroenamide was established.（?）In Chapter 3,The preparation and properties of cyanoaryl substituted enamines were studied.Using polyhalogenated 1,3-m-phthalonitrile and ethyl pyridineacetate derivatives as raw materials,water as green solvent,Et3N as base,refluxing reaction for 9 hours,Cyanoaryl substituted enamine ester heterocyclic compounds were synthesized by regioselective nucleophilic substitution reaction,with the yield of 71-93%.The results of antitumor activity screening showed that compounds 3d and 3n had good antitumor activity in vitro.（?）...