Research On Synthesis Of Allenes And Ynamides With Biological Activity

Objective Allenic compounds species less in nature, it is difficult to extract the separation. So use a new synthetic method, simple and efficient synthesis of biologically active allenic compounds. There is a great help for the study of allenic compounds of biological activities and pharmacological effects. Ynamide play an important role in organic chemistry, so explore a new method to synthesis it is very significantly.Methods In this paper, the preparation of propargylic alcohols and hydrazone compounds with simple and efficient system of substrate.The reaction conditions were optimized.Propargylic alcohols and hydrazone compounds, generated with 1,3-allenols with propargylic alcohols in the catalytic reaction of CuI and tert butyl lithium. The allene fragment into natural products and drugs provide a new method. What’s more, the propargylic alcohols and vinyl azides compounds under BF3Et2 O catalysted, synthesized lots of ynmides.Results Under the optimum conditions, the synthesis of a variety of functional groups substituted 1,3-allenols and ynamides. The electron withdrawing groups or containing electron donating groups, obtained the target product in good yield.Conclusions Propargyl alcohol is a kind of functionalized alkynes with high reaction activity, hydroxyl andcarbon carbon triple bond is directly connected with the reaction of propargyl alcohol The hydrazone compounds are good carbene precursor, vinyl azides also have a activity structure. In this paper, development of two new synthetic methods use propargyl alcohol reacted with hydrazone and vinyl azide. In simple conditions, synthesized the biologically active compounds allenols and ynamides.Two methods have the characteristics of simple operation, low raw material cost, atom economy. Provided a good research with allenols and ynamides.