Part I: Design And Synthesis Of Cardiovascular Activity Of Natural Product Derivatives Part II: Synthesis Of Rivastigmine Bitartrate Related Substances

In this paper, two parts are included:design and synthesis of derivatives for cardiovascular and cerebrovascular disease, and synthesis of the related substances of Rivastigmine Tartrate.The First Part:Design and synthesis of derivatives for cardiovascular and cerebrovascular diseaseCardiovascular and cerebrovascular disease is a serious threat to human, especially to the old people. The most important reason of cardiovascular disease is atherosclerosis, and hyperlipidemia is the pathological basis of atherosclerosis. Therefore, reducing blood lipids is important to prevent and treat cardiovascular and cerebrovascular diseases. The research group took cordycepin as lead compound, and discovered the compound WS070117with lipid regulating activity. Then treating WS070117as lead compound, we design and synthesis13derivatives. The results of animal experiments show that some compounds have good lipid regulating activity. The incidence of ischemic disease occupies the first place in cerebrovascular disease, and neuroprotective agent is a large class of the drugs which have potential applications for the treatment of ischemic cerebrovascular disease. The previous research found that compound PN1which was derived from curcumin exhibits neuroprotective activity. We take compound PN1as lead compound, design and synthesis34derivatives. The activities of all derivatives are under biological evaluation. All of the derivatives were confirmed by MS and NMR.The Second Part:Synthesis of the related substances of Rivastigmine TartrateRivastigmine tartrate is an acetylcholinesterase inhibitor and used for the treatment of mild and moderate Alzheimer’s disease. To perform the quality control of the bulk drug and drug formulations, it is necessary to prepare the related substances of the drug. According to the Rivastigmine’s structural feature and its synthetic route, the author synthesized8related substances, and the amount of each substance was more than1gram. The chemical structures were confirmed by HRMS,1H NMR,13C NMR, and their purities were content for a variety of drug quality control.