一种盐酸胍甲环素的合成方法

A Method of Synthesis of Guamecycline Hydrochloride

盐酸胍甲环素又名盐酸胍哌甲基四环素,为四环素类广谱抗菌素,其抗菌谱和抗菌作用与四环素类似,对肺炎球菌、乙型链球菌等活性较强。我们通过六水哌嗪与双氰胺进行加成反应得到中间体盐酸哌嗪双胍,然后其与盐酸四环素及甲醛进行缩合反应得到盐酸胍甲环素纯品;该工艺路线总收率达到了35.9%,反应条件温和,使用反应溶媒较为绿色(酒精),实现了反应的绿色减排,同时具有反应路线短等优点,显著降低了该产品的工业生产成本,使其便于工业化生产。

Guamecycline Hydrochloride,also known as guanidinium tetracycline hydrochloride,is a tetracycline broad-spectrum antibiotic.Its antibacterial spectrum and antibacterial effect are similar to tetracycline,and it has strong activity against pneumococcus and streptococcus b.We obtained the intermediate piperazine biguanide hydrochloride by the addition reaction of piperazine hexahydrate and dicyandiamide,and then condensed it with tetracycline hydrochloride and formaldehyde to obtain the pure product of guamecycline hydrochloride;the total yield of the process route reached 35.9%,the reaction conditions are mild,the reaction solvent is relatively green(alcohol),which realizes the green emission reduction of the reaction,and has the advantages of short reaction route,which significantly reduces the industrial production cost of the product and makes it convenient for industrial production.