The Preparation And Research Of5-fluorouracil N1Substituted Derivatives

Uracil derivates are important constituents of organism genic materialsand DNA and RNA. Lots of them have different biological activity, and theyare prodrug and intermediate compounds of many medicines, thus they areused in antitumor drugs clinically. Today, a lot of antitumor medicines aresynthesized and screened by the molecular modification such as insertingmolecular, metal atoms in biologic and chemistry.In this paper, we try to modify the uracil derivates by many methods,such as esterification acidylation and coupling reactions of C-N. We havesynthesized and screened some activated compounds and investigate abouttheir activity. The paper makes up of four parts. Firstly,5-floururacilderivates react with phenylamines to synthesize acylamide through thecatalyst of DIC, and characterize their chemical structure and biologicalactivity. Secondly, prepare and characterize a series of ester compounds byesterification reaction catalyzed by DIC, Thirdly, via the green and efficientMichael addition reaction, we prepare some1N-C coupling compounds byusing uracils and acrylic ester as materials. Finally, using uv spectra andfluorescence spectrometry, we have determined the reciprocity of parts ofcompounds and DNA and BSA, besides, have got the force constant ofbinding constant (Ka) and binding site(n).In a word, about the molecular modification of uracils is the focus ofresearch in my group. This paper introduces the convenient efficient method to prepare and characterize uracil derivates. Besides, via the research thecompounds’ biological activity, we can offer foundation as the theoretical andactivity research about the uracil.