Synthesis Of 5,6-member Heterocyclic Compounds Using Multi-component Reactions

5,6-member heterocyclic compounds are very active in the fields of chemistry, biology and material science. Multi-component tandem reactions are convergent reactions, which are the frontiers of organic chemistry and the hot spots. It is obviously very important of good research and application of value to synthesis the 5, 6-member heterocyclic compounds by using efficient multi-component tandem reactions.This paper mainly discussed the multi-component tandem reactions, reported the works of the synthesis of 5,6-member heterocyclic compounds, using multi-component tandem reactions, the main contents are as fellows:1. Synthesis of 3,6-2H-1,3-oxazine derivatives.1,3-oxazine derivatives have a variety of biological activities. On the basis of a comprehensive discussion of 1,3 and 1,4-dipole cycloaddition reactions, we reported a new type of dipolar cycloaddition reaction, which is three-component reaction ofα,β-unsaturated imine, acetylenedicarboxylate, aromatic aldehydes, one-pot efficient synthesis of highly-functional 1,3-oxazine derivatives.The structures of the 34 new compounds in total were characterized by 1H NMR,13C NMR, IR and HRMS. This method does not require a catalyst or any other additives, with simple operation and a good yield (36-97%) of 1,3-oxazine derivatives at 50℃or even at room temperature.2. Synthesis of the precursor of F-labeled kinesin spindle protein (KSP) inhibitors. The bi-functional compounds of diagnostic and treatment drugs have a very broad application and important theoretical value. This chapter is mainly about the synthesis of 5,6-member heterocyclic compounds, using the Biginelli and Povarov multi-component tandem reactions. The synthetic precursors of these KSP inhibitors have laid a good foundation for 18F-labeled inhibitors and medical research.