新型抗菌药物头孢洛扎关键中间体UBT的制备方法

A method for preparing the key intermediate UBT of a novel antibacterial drug ceftolozane

本论文进行了抗菌药头孢洛扎关键中间体UBT的制备方法研究。首先将起始原料1-甲基-5-氨基-4-乙氧羰基吡唑与三苯基氯甲烷反应得到中间体1;然后中间体1在碱性条件下进行水解反应得到中间体2;最后中间体2通过与DPPA、BocEDA一锅法反应制备得UBT。本工艺得到的UBT总收率及纯度较高,原料易得,适合工业化生产。

A method for preparing the key intermediate UBT of an antibacterial drug ceftolozane was studied in this paper.The starting material 5-amino-1-methyl-1H-pyrazole-4-carboxylic acid ethyl ester was reacted with the triphenylmethyl chloride to obtain intermediate 1.Subsequently,the hydrolysis reaction of intermediate 1 was accomplished under basic conditions to synthesize intermediate 2.Finally,the UBT was prepared via the one-pot process with DPPA and BocEDA.UBT in high purity and yield was prepared via the process.Furthermore,the raw materials of this process were easy to obtain.The process could thus easily be scaled up to an industrial process.