Three-Component One-Pot Synthesis Of Benzopyran [4,3-d] Pyrimidines And Bicyclic Pyridines

Heterocyclic compounds,especially N-containing heterocycles,often have good drug activity.There are N-containing heterocyclic structures in many natural drug molecules,such as vitamins,hormones and antibiotics.Benzopyran[4,3-d]pyrimidine derivatives have good antiplatelet activity,and have good clinical application prospects in the treatment of thrombotic diseases.Bicyclic pyridine derivatives have antithrombin activity,and can also be used in the clinical treatment of thrombotic diseases.Therefore,it has high application value in the synthesis and activity research of benzopyran[4,3-d]pyrimidine derivatives and bicyclic pyridine derivatives.In this paper,green and efficient synthetic methods of these two kinds of heterocycles were developed through literature research.In the first chapter,the pharmaceutical activities and synthesis methods of benzopyran,pyrimidine,benzopyran[4,3-d]pyrimidine derivatives and bicyclic pyridine derivatives were reviewed.In the second chapter,a three-component one pot green and efficient method for the synthesis of benzopyran[4,3-d]pyrimidine derivatives was established.A series of benzopyran [4,3-d] pyrimidine derivatives were synthesized by using heterocyclic ketene aminals（HKAS）,formamidine hydrochloride and 3-formylchromone as raw materials,acetonitrile as solvent,Cs2CO3 as base,heating at 80 ℃ for 3h with 64-86% yields.In the third chapter,a series of bicyclic pyridine derivatives were obtained by refluxing the mixture of HKAs,enaminones and 3-formylchromones in acetonitrile and promoted by Cs2CO3 for 2 hours.The yields were 59-76%.