The Design And Synthesis Of Novel Quinoiine Derivatives Containing N-phenyl Piperazine

Heterocyclic drugs are an important class of compounds, mainly because of theirphysiological activity of bicyclic and tricyclic derivatives. Wherein the1,5-benzothiazepine derivative, and is a type of his more famous N and S-containingseven-membered heterocyclic ring. This is mainly because they have broad biologicalactivity, e.g., antibacterial, anti-HIV, calcium antagonists, analgesic andanticonvulsant activity. For example, the drug is widely used in clinical-diltiazem,and to contain the system. Currently,1,5-Research benzothiazepine derivatives manydrugs have become a hot research chemists. In addition, as a calcium antagonists,theyare the main ingredient in many important analgesics drugs.In the pharmaceutical industry, many of quinoline compounds are importantpharmaceutical intermediates. Recently, many novel quinoline ring-containing drugsare constantly developed, but also from the quinoline antimalarials itself originallyquinine is obtained by distillation. The main application of synthetic antimalarialdrugs, such as quinoline up malaria, chloroquine phosphate, phosphoric acid andacetaminophen primary amine quinoline quinoline; local anesthetic dibucainehydrochloride drugs; anti-inflammatory drugs Xin can be fun; antibiotic drugsdequalinium; anti-Arab Miba quinoline iodoform disease drug, clioquinol, iodoquinolso on. The quinoline ring flutter can be synthesized and other heterocyclic Nao Lingand Xie Li Ning grams. Through the previous studies, we found that the1,3-dipolarcycloaddition reaction could build the four-membered heterocyclic ring and thefive-membered heterocyclic ring successfully. During the study, we introducing thequinoline ring into the1,5-benzothiazepine nucleus in order to get the biologicalactivity of the compounds those we want to desired.Our main job is introduced the N-phenyl-piperazine substituted into the quinolineheterocyclic molecules, and by the1,3-dipolar cycloaddition reaction，we aresynthesis and design a series of novel containing N-phenyl-piperazine quinolinederivatives successfully.This thesis is divided into two parts:The first part of the literature review section:This part of the quinoline,1,5-benzothiazepine,1,2,4-oxadiazole synthesismethods as well as physiological and pharmacological activity of the situation athome and abroad in the study were relatively systematic exposition; It also briefly describes the1,3-dipolar cycloaddition reactions on1,5-benzothiazepine derivativesand quinoline-containing1,2,4-oxadiazolines structural modification of derivativescyclization.The second part is the experimental section, the main work is as follows:1, The synthesis and characterization of novel quinoline derivatives ContainingN-phenyl piperazine of its derivatives1,5-benzothiazepines with α-chloro oxime by1,3-dipolar cycloaddition reaction of a series of1,2,4-oxadiazole and1,5-benzodiazepine class derivatives.2, The synthesis and characterization of new quinoline containing N-phenylpiperazine and1,2,4-oxadiazolines derivatives2-(4-Phenylpiperazin-1-yl)quinoline-3-carbaldehyde with formaldehyde to givethree kinds of different reaction imine, imide, and then four kinds of α-chlorooximeby1,3-dipolar cycloaddition reaction of a series of quinoline-containing1,2,4-oxadiazolines derivatives.3, The synthesis and characterization of Novel quinolyl1,3,4-OxadiazolinesDerivatives containing N-phenyl piperazine2-(4-Phenylpiperazin-1-yl)quinoline-3-carbaldehyde with different substitutedbenzoyl hydrazine to give a series of new acylhydrazone then acetic anhydrideoxidative cyclization to give a series of novel quinolyl containing1,3,4-oxadiazolinesderivatives.The product structure were characterized by elemental analysis, MS, IR,1HNMR and13C NMR, then its spectral properties was analized and discussed.