Tazobactam Production Technology Research And New Synthetic Method Of Amino Alcohols From Cyclic Ethers

Tazobactam production technology:Tazobactam is a kind of β-lactamase inhibitors which is widely used, when it is used with other antibiotics, we can see its advantages such as high antibacterial activity and low resistance. There are many problems in its production technology, such as low yield of product and lots of byproducts in the important steps. This thesis shows the researches on the problems of the production technology of tazobactam. Meanwhile in this thesis we have successfully solved some of the problems and study some key steps from theory. In the researches, we have gained some achievement:First, we improved the bromination reaction and the oxygenizement reaction, enhanced the yield; Second, improved the esterification reaction, discover the influence of different substituent groups on the reaction; Third, established the High Performance Liquid Chromatography conditions of the key steps, which played an important role when we monitored the yield of the reaction and the extent of reaction in laboratory; Fourth, we improved the temperature and the solvent of the ring opening reaction, the yield of the reaction was enhanced and the conversion rate was increased; Fifth, we did researches on the factors of the azido reaction to find the optimum conditions which would contribute to more main product; Sixth, we improved the production technology of tazobactam on the whole, enhanced the yield of the reaction.New synthetic method of amino alcohols from cyclic ethers:Through the researches on the synthesis of amino alcohols which used tetrahydrofuran and 2-methyl tetrahydrofuran or other cyclic ethers with different kinds of amines, we found a few common features which existed in these reactions. Some of these reactions are useful in the synthesis of the side chains of chloroquine and hydroxychloroquine.