The Total Synthesis Of(+)-JQ1 And Tripdiolide

This paper mainly introduces the background of(+)-JQ1 research,synthesis of the status quo and our synthesis method and tripterygium wilfordii b background research and synthesis of our research.This paper mainly divides into the introduction,the synthesis of(+)-JQ1 research and the synthetic study of tripterygium wilfordii b element this three parts.The first chapter introduction(+)-JQ1 is a new kind of thiophene and triazole-1,4-two of mixed nitrogen grass,with an additional in C6,huge sihuan tert-butyl ester functional groups of compound.Bromo,it is the first structure of a domain from the crystal structure of bundling sunken mouth candidate ligand molecular model.It on the treatment has a significant effect in the human squamous cell carcinoma.It has again in HIV-1 transcription activation,the effect of inhibiting T cell proliferation and induce gene and potent inhibition of histone modification of the genes involved in T cell activation again.Now many scientists are still doing its biological activity test,believe that it must have been very broad application prospect.Has published a synthesis method of Panagis Filippakopoulos group in 2010,published in the journal NATURE and Bradner group published in 2011,the PCT Int.J Appl.These two kinds of synthesis methods.As its importance reflected,later will have more better method was developed.The second chapter,the synthesis of(+)-JQ1 researchOn the basis of literature research,we found(+)-JQ1 is a cell cancer and effective drug in the treatment of HIV-1 small molecules.We are on the basis of previous studies,by improving the method and procedure,use more simple steps,a total of six steps,the overall yield was 4.66%of the route of(+)-JQ1 synthesis again.This not only save raw materials and cost,but also provides a reference value for the mass production.Because we consider the(+)-JQ1 than its enantiomorphism isomers(-)-JQ1 better curative effect in cancer cells,so we selective synthesis of(+)-JQ1 only,for its application in biomedical to provide more opportunities and conditions.But at the same time,we also see the improved method steps are still more,we will continue to improve in the future work.The third chapter the synthetic study of tripterygium wilfordii b elementTripterygium wilfordii b is one of the more than tripterygium wilfordii glycosides,it has anti-tumor,anti-inflammatory,suppress the immune response and the activity of anti fertility effect effect.We in tripterygium wilfordii a synthesis and research on the basis of the relevant literature,studied the synthesis of tripterygium wilfordii b,.We can buy from the raw material,after eight steps to a key intermediates,but encountered difficulty in synthetic steps back.We have done a lot of trying,there is no the step response in the past.To this end,we are trying new synthetic route,the relevant work continues.