Research Of1,3-dipolar Cycloaddtion In Synthesis Of Aryl Spiroheterocycles And Green Synthetic Of Drug Intermediates

Spiro compounds are a class of natural products and drugs in commonheterocyclic compounds，which have a variety of biological activities in medicineantibacterial，antiviral，anti-inflammatory and other biological activity，now it is a hotresearch topic.1,3-dipolar cycloaddition reaction is an important organic synthesisreaction，its application is very wide and played a crucial role in the synthesis of avariety of drug intermediates.In this paper，use1,3dipolar cycloaddition and click chemistry to synthesizesome aryl spiro compounds and improved green synthesis of a number ofpHarmaceutical intermediates.Chapter1: The Systematically describes the synthesis of spiro compounds，theapplication and development of1,3-dipolar cycloaddition，and conducted a series ofsynthesis of aryl spiro compounds and their characterization.Chapter II:4-methyl-2-benzothiazole hydrazine is the major industrialintermediates currently used to synthetic broad-spectrum fungicide Tricyclazole.Summarized synthetic methods，based on this，we proposed an effective method tosynthesize this product. This chapter describes the use hydrazine water as a solventwith Aminobenzothiazole，under high pressure environment，the process is simple tooperate，the treatment is simple，having a better social and economic benefits，suitablefor industrial promotion.Chapter III: methylation of the pHenol is an important class of organic syntheticmethods. usually use methyl halide or dimethyl sulfate as a methylation reagent，it notonly the treatment after the reaction waste volume and reagent itself has serious toxicand carcinogenic risk，not meet the needs of sustainable development. This chapterdescribes the dimethyl carbonate (DMC) which good for the environment as amethylation reagent to synthesize some of the drug intermediates. As the methylatingagent，methanol and carbon dioxide is the only reaction by-products after reaction，they can be easily removed from the reaction medium.