Synthesis Of The Compounds Of Phenylporphyrin-5-Fluorouracil-1-acetic Ether

5-Fluorouracil is a kind of popular antimetabolic drug used in clinic.It has the similar structure with uracil which is necessary to the cancer cell.It contents with uracil in the same enzyme system,blocks the metabolic link,impeds the synthesis of DNA,and then prohibits the propagation of the cancer cells.As a kind of antitumor drug,5-Fluorouracil has inhibition effect on many kinds of cancer,but it also seriously hurts the normal cells while it kills the cancer cells. The half life time of 5-FU in vivo is only10-20minutes and its bioavailbility is very low.Continuous infusion was commonly used to maintain long-time steady concentration. Its these shortcomings limit its application of clinic. In recent years,many chemists have modified their chemical structures and hope to develop a better drug to overecome its shortcomings.In order to improve the target activity of anticancer medicine and reduce their untowa- rd effects,the effective drug is expected with high selectivity,which means it can distinguish target cell from normal cell properly. Phtodynamic therapy(PDT) is newly developed treatment for tumor since the 20th century.Porphyrin and metalloporphyrins have special affinity with cancer cell because their distinctive structure.They can be taken up and retained by tumor tissue selectively.With the appropriate light,they can produce fluorescence and kill the cancer cell.So the research on the use of porphyrin and metalloporphyrins for tumor localization and therapy have caused great interests of chemists,medicals and biologists.In order to improve the lipophilicity and half life time of 5-FU,we synthesize 5-Fluo- rouracil-1-acetic ether .As the same time in order to decrease the toxicity of 5-Fluorouracil,we synthesized a series of porphyrin-5-Fluorouracil-1-acetic ether compounds.We expected these compounds can reach tumor tissue directly and kill cancer cell,so as to improve the curative effect.Furthermore, they cure cancer coordinating laser technology at the position of the body which the laser can reach for better curative effect.In this paper,we synthesized and charactered six porphyrin-5-Fluorouracil-1-acetic ether compounds. The results are as follows:In the first part, six porphyrin-5-Fluorouracil -1-acetic ether compounds have been prepared.That is,Phenylporphyrin substituted by different organs and 5-Fluorouracil-1-acetic ether were linked up by different bonds.The structures of six porphyrin-5-Fluorouracil- 1-acetic ether compounds have been characterized by UV, IR, 1HNMR and MS.In the second part ,optimum reaction and separaion conditions have been reaserched and improved...