Synthesis Of The Novel Heterocycle-Fused Pyridines Via P-S Cyclization

In this paper,pyridine rings were used as the research object.By Pictet-Spengler reaction,a more efficient,highly selective synthesis method was identified and synthesized a series of pyridine fused heterocyclic compounds.Firstly,disscusses the biological activities of pyridopyrimidinone comp ounds and pyridinecoumarin compounds,and summarizes their synthesis m ethods.Introduces the Thorpe-Ziegler reaction and Pictet-Spengler reaction.By summarizing the work of the laboratory for many years and the basic synthetic route of this paper is proposed.Secondly,this paper describe that using the 2-chloromethylpyridopyri midin-4-one as the starting material and two novel pyridopyrimidone inter mediates obtained by Thorpe-Ziegler reaction through reaction with phenyl isothiocyanate and malononitrile(or cyanamide).Using this intermediate as material,discusses the Pictet-Spengler reaction with aldehydes under th e action of p-toluenesulfonic acid and the thieno(or thiazol)-pyrido-pyrido-pyrimidinones compounds was synthesized.Finally,this paper describe that using the 4-chloromethyl-7-methylco umarin as the starting material and two novel coumarin intermediates obta ined by Thorpe-Ziegler reaction through reaction with phenyl isothiocyanat e and malononitrile(or cyanamide).Using this intermediate as material,di scusses the Pictet-Spengler reaction with aldehydes under the action of Tri fluoromethanesulfonic acid and the thieno(or thiazol)-pyrido-coumarin com pounds was synthesized.