Research Of Solvent-free, Catalytic Synthesis Ofα-amino Phosphonate Derivatives With TMSCl

As the stucture of α-amino phosphonate derivarives is similar to natural amino acids, this compound play an important role in the field of biology and pharmacology, α-amino phosphonate derivative inherited the good bioavailability properties from the natural amino acid, it shows low toxicity and low residual amount, generally, it is used as insecticides, herbicides, fungicides, growth-regulating agents, enzymes inhibitors, and even can be used as anti-cancer drugs and antiviral drugs. So the a-amino phosphonate derivatives have attracted much attention, and an efficient synthetic method of α-amino phosphonate derivatives is very important.Nowadays, α-amino phosphonate derivatives are applied widely, and there are lots of synthesis methods of α-amino phosphonate derivatives. The efficient systhesis method of α-amino phosphonate derivatives is very important, and the most famous synthetic method is two-step synthesis method, which use an organic solvent method. But this method have some disadvantages, such as the final product extraction is difficult, low yield and some environmental issues. In this case, this paper proposed a " one-pot" synthesis method to synthesize a new solvent-free product. This paper describes a new method that use trimethylchlorosilane (TMSCl) as synthesis catalyst for solvent-free synethsis, the product is a series of α-amino phosphonate derivatives.Firstyly, in the solvent-free react system, the use of substituted benzaldehyde, substituted aniline and diethyl phosphite as raw materials, and TMSCl as a catalyst, the "one-pot" synthesis method has been used to synthesized a series of α-amino phosphonate derivatives. Furthermore, this paper also analysed the effect of TMSCl concentration and the ratio of raw materials for the yield of synthetic products. Finally, the structure of representative compoud were tested by X-single-crystal,’H NMR and 13CNMR. It is indicated that this synthesis method is a gree synthetic method with mild reaction conditions, the convenient way of operation, high yields and environmental friendly.Secondly, the second chapter is on the basis of experiments in the first chapter, to explore a kind of new type2-amino benzothiazole derivatives were synthesized.2-amino benzothiazole derivatives are used as herbicides, fungicides,growth regulators, enzyme inhibitors, and even can be used asanticancer and antiviral drugs. Therefore2-amino benzothiazole derivatives synthesis method with high efficiency has attracted a lot of attention.2-amino benzothiazole derivatives in now use is very extensive, and the synthetic method of many. Many synthetic method is through the concreteis:the intermolecular and molecule at the tour de france.In this paper, the synthesis method of two. The first part:2-aminobenzothiazole in catalytic synthesis of formaldehyde and formic acid (2-aminobenzothiazole) methanol; second:using N, N-double tert butylamino phosphite as catalysts for the synthesis of2-amino benzothiazole derivatives. Finally, their structures were confirmed by 1HNMR,13CNMR and mass spectrometry, the synthesis method of mild reaction conditions,convenient operation, high yield and is friendly to the environment, is a kind of method for the synthesis of green.