Preparation method for pidotimod

Abstract

The invention relates to a preparation method for pidotimod. The method comprises the following steps: synthesis of L-thiazolidine-4-formic acid, preparation of metal-ion-loaded type cation exchange resin and synthesis of the pidotimod. The invention has the following beneficial effects: with metal-ion-loaded type strong acid cation exchange resin as a catalyst, and L-cysteine and L-pyroglutamic acid as raw materials, pidotimod is directly synthesized under the action of the catalyst, so the number of synthetic reaction steps are shortened from conventional four steps to two steps; the total yield of the pidotimod is increased from conventional reported 55% to 64%; and through HPLC detection, the content of the pidotimod reaches 98.5%; meanwhile, substances with great toxicity are prevented from being used in reaction process, and a solid catalyst is used, so synthesis process is safer and more environmentally friendly, and product purity is guaranteed.

Description

technical field [0001] The invention relates to a preparation method of pidotimod, which belongs to the field of chemical synthesis. Background technique [0002] The chemical name of pidotimod is (R)-3-[(S)-(5-chloro-2-pyrrolidinyl)carbonyl]-thiazolidinyl-4-carboxylic acid, which is an immune Regulators, first launched in Italy in 1993, are mainly used for the prevention and treatment of children with recurrent respiratory tract infections, urinary system infections, allergic rhinitis and asthma, and for the treatment and prevention of acute exacerbations of chronic bronchitis and upper respiratory tract infections. They can also be used for a variety of viruses Infections, malignancies, and other chronic diseases result in a weakened immune system. [0003] The existing synthetic method of pidotimod is to use L-cysteine ​​and L-pyroglutamic acid as starting materials, after acylation or esterification reactions to generate corresponding intermediates, and then the two int...

AI Technical Summary

Problems solved by technology

However, due to the low activity of the acylating agent and the acylated product in the N-acylation reaction, and the presence of other active groups in the reactant that have side reactions, the yield of the N-acylation reaction is low, which directly results in the synthesis of acylated compounds. Domod's overall yield is low

In order to improve the yield of N-acylation reaction, some processes have adopted different methods on the raw materials of N-acylation reaction (i.e. the synthesis of intermediates) and the catalyst of N-acylation reaction, but there are still raw materials with high toxicity. Shortcomings such as instability of intermediates

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