Industrilization Of Aminoglycoside Antibiotic Arbekacin

Aminoglycoside antibiotics are mainly used to treat bacterial infections caused by Staphylococcus aureus and aerobic gram-negative bacteria.It is considered to be the last line of defense against bacterial infection.At the same time,aminoglycosides also have the effect of targeted treatment of HIV.Due to the abuse of antibiotics,bacteria also gradually develop drug resistance.The reason of bacteria reproduce and produce certain drug resistance is that there are aminoglycoside modifying enzymes in bacteria.These enzymes will modify the active sites of aminoglycoside antibiotics and reduce their antibacterial activity.Therefore,in order to resist bacterial drug resistance,a series of semi-synthetic aminoglycoside antibiotics were born.Among them,Arbekacin is known as an extremely important aminoglycoside antibiotic in the21 st century because of its small toxic and side effects,low drug resistance and wide antibacterial spectrum.The drug has been used in more than 250000 patients with good clinical benefits and safety.Abekacin is classified as an aminoglycoside antibiotic of kanamycin family,which can cause bacterial cell membrane damage and bind to 30 S ribosomal subunit,causing codon misreading and inhibiting translation in the process of transcription.Due to the long synthetic route and complex process of Arbekacin,it has not been listed in China.In order to fill the market vacancy and realize the effective utilization of kanamycin B,the by-product of Kanamycin A fermentation,this subject optimizes and improves the existing patent route to realize the green,environmental protection and high yield synthesis of Arbekacin.The industrialization research and process optimization of the synthesis process were carried out to realize the kilogram amplification of intermediate Dibekacin and the hundred gram amplification of Arbekacin,and the related substances produced in the production process were studied to prepare for the industrialization of Arbekacin.