| abstract |
The invention discloses a kind of methods preparing full substituted amidine, using sulfamide derivative, carbonitrile derivatives and diazo compound derivative as reaction substrate, using transition metal as catalyst, in organic solvent, full substituted amidine are prepared by four component cascade reactions.Method used in the present invention has the characteristics that：React that more economical, substrate universality is wider, later stage function dough is more easy to, avoids the waste of raw material, reaction condition is mild, can be carried out in air, and catalyst amount is few, and post-processing is easy, is conducive to purifying and the heavy industrialization application of product.Simultaneously, the raw materials such as reactant, catalyst that the present invention uses are cheap and easy to get, reaction composition is reasonable, is not necessarily to ligand, and Atom economy is high, reaction step is few, it only needs single step reaction that can obtain higher yield, meets contemporary Green Chemistry and pharmaceutical chemical requirement and direction, be suitable for screening the amidine class drug of high activity, gram-grade reaction can also be realized well, be suitable for large-scale industrial production. |