9 - Hydroxy Xanthene Carboxylic Acid Esters Were Designed And Synthesized

Anticholinergic drug is an important neural drug, which can be used to cure poisoner and be applied to first aid drugs. In civil life, it can cure parkinsonism, car sickness, seasickness, stomach convulsion and gastric ulcer. In military affairs, it can entreat the raid of chemical arms. Thereby, it is regarded as drugs of antiterrorism to overmaster terrorist. In addition, it can be applied to the study of the mechanism of antiuscarinic and antinicotinic activity.Chapter 1 introduced the progress of anticholinergic drug and the synthesis of aim compound. First, anticholinergic drug was extracted by natural medicine. Now, people pay more attention to the synthesis of anticholinergic drug. But the side-effect of drug and poor efficacy become a chief difficulty . Therefore searching for good effect, high selectivity and quick function drug is one of the hotspots. Anticholinergic drug is composed of interaction group, link group and cation group. In this paper the synthetic route is devised to three parts-the synthesis of 9-hydroxyl-carboxyl ester, N-substitute-piperidines and target compounds respectively.Chapter 2 introduced the synthesis of xanthene carboxylates. Originaly xanthene carboxylates was synthesized with 9-hydroxyl xanthene carboxyl acid, but the material was limited. Afterword, it was synthesized with chloromethane acid, however the reactive yield was too low. In this paper, 9-xanthene carboxyl acid is used to synthesize 9-hydroxyl xanthene carboxyl esters by interesterification.Chapter 3 introduced that 9-hydroxyl xanthene carboxyl ester is synthesized by microwavecatalysis. Under traditional reaction conditions, the reaction time is 18 hours. In order to shorten the reaction time, microwavecatalysis is made use of synthesizing mass target compounds. By orthogonal design, the optimal synthetic condition was formed in the microwavecatalysis.Charter 4 introduced the structure-activity relationship of xanthene anticholinergic drug and the gauss calculation. By gauss calculation, this paper investigated the relation of interdiction group, cation group and the energy of HOMO, the energy of LUMO, thedensity of charge. Effects on activities of xanthene derivatives by interdiction group and cation group were discussed.Chapter 5 reviewed the synthesis, microwavecatalysis and structure-activity relation in this paper. The design of anticholinergic drugs is prospected.Chapter 6 introduced the study of solid-substrates room temperature phosphorescence(SS-RTP). Polycyclic aromatic hydrocarbons(PAH) and Nitrogen heterocyclic compounds(NHCs) were determined by synchronous scanning with solid-substrates room temperature phosphorescence(SS-RTP).Synchronous scanning spectrums were obtained using potassium iodine as heavy atom salt perturbation and β-cyclodextrin modified filter paper as solid substrates. Some conditions were examined, including drying time(t=5min), heavy atom (V=7μL)and the constant wavelength interval (△λ=150nm). Linearity range is 6.30ngmL^-1～1.67μg-mL^-1 with limit of detection 6.30ngmL^-1.The precision (RSD=2.59%) was satisfied. The method is convenience and rapid without separation.