Construction The Core Of Several Natural Products Via Alkylated Derivatives Of Acetoacetarylamides

It is well-known that the green chemistry and chemical-saving are direction of the current organic synthetic chemistry. How to use cheap, readily available reagent to facile and efficient synthesis of useful compounds for humans is a major problem, which needs to be considered for chemical workers in the experimental design and the implementation process. Acetoacetarylamides and its derivatives are important reagents in organic synthesis. They have more active sites and a wide range of applications, especially in the dye industry and pharmaceutical chemistry. Acetoacetarylamides and their derivatives chemistry have also been more perfect than ever in a century of research, so developing efficient and atom-economy chemistry is worth the wait.This paper mainly discusses the new applications of acetoacetarylamides and its derivatives in organic synthesis, including their preparation and reactions of common derivatives, and also detailed the preparation of several important core of natural products by the intramolecular tandem reaction of readily available acetoacetarylamide alkylated derivatives on the basis of the literature and our previous work, these mechanisms were also in-depth study. We believe that these findings can be theoretical guidance for the synthesis of other heterocyclic compounds. During the specific research process, we mainly have completed the following two tasks: 1) we determined the optimizing conditions through screening of the catalyst, solvent, temperature etc., and several series heterocyclic compounds were synthesized under optimal conditions. 2) In order to provide a theoretical support for synthesis of other heterocyclic compounds, the reaction mechanisms were in-depth studiedThe traditional synthesis of fused-heterocyclic compounds are often require multi-step, not only needs a long time and the total yield of the products increases due to multi-step reaction. It is quite a challenging task for the synthesis of the core structure of valuable natural products by functionalized acetoacetarylamide derivatives. In contrast, the advantages of our synthesis are:(1) Ready-made, low-cost raw materials: Acetoacetarylamides are important chemical raw materials, synthetic simple, cheap, and very convenient for transport and storage.(2) Easy preparation of functionalized derivatives: Preparation of the series of alkylated acetoacetarylamides is one-pot protocol by using acetoacetamides, alkali and haloalkanes under mild conditions. the reaction is easy to control and the product yield is satisfactory, easy separation and storage.(3) High selectivity and high yield: The reaction showed high chemical selectivity, regioselectivity and high yield during the fuseheterocyclic synthesis process via functionalized derivatives of acetoacetarylamide.(4) High atom economy: we obtained some of heterocyclic moleculars by high atom economy from a series of simple functionalized derivatives of acetoacetarylamide. All the atoms of raw materials are almost retained in the product, the only by-product is water. We achieved the greatest atom economy.(5) Provide theoretical guidance to synthesize other heterocycles: We have made full use of functional groups of alkylated derivatives of acetoacetarylamide to build fuseheterocyclic derivatives by domino reaction with highly regioselective. This method may provide a novel and common methods for synthesis of heterocyclic compounds. And aslo, it can provide a theoretical basis for the synthesis of other heterocyclic compounds.