Investigation On The Synthesis Of Pidotimod:an Immunomodulating Agent

Pidotimod is a new type of synthetic immunomodulator.It owns a variety of advantages compared to the traditional biological regulator,such as being absorbable,safety,few adverse reactions,no accumulation effect,and high durability.Therefore,the synthetic immunomodulator has a broad market prospect.This paper is divided into three chapters: Chapter 1 briefly introduces the classification of immunomodulator and their current market situation.Firstly,Chapter 2 briefly introduced mechanism of action of ph-armacokinetics,clinical applications and market situation of pidotiod.Secondly,its synthetic routes were researched and both advantages and disadvantages of synthetic methods were analyzed,which provided the theoretical basis for the synthesis of pidotimod.In chapter 3,two synthetic routes are designed on the basis of the existing literature methods.The reaction conditions at each step of the process were investigated and the optimum reaction conditions for each reaction were determined.By comparing route one is better than route two,The details are as follows: L-thiazolidine carboxylic acid is prepared via addition of L-cysteine and formaldehyde,then carboxyl protection into ester,further condensation with the L-pyroglutamic acid by condensing agent,and finally,pidotimod is given by hydrolysis.The recovery of the condensing agent and the catalyst was tested,the results showed that the recovery yield of the condensing agent was low but the catalyst recovery yield was high.In addition,the peptide solid phase and strong acid cation resin synthesis of pidotimod were attempted,the comparative analysis shows that strong acid cation resin synthesis method of short route,simple operation,and peptide solid-phase synthesis for the carboxyl protection provides new ideas.The synthesis method is designed in this paper has many advantages,such as being environmentally friendly and easy to obtain with low cost,stable intermediates and convenient operation,so its application prospect is promising.