Synthesis method and application of free-state single-molecular-weight amino-polyethylene glycol-propionic acid

Free amino-polyethylene glycol-propionic acid can be directly prepared by synergistic catalysis of cerium chloride heptahydrate and sodium iodide under neutral conditions. This method solves the problems of cumbersome processes and difficulty in controlling product morphology in existing technologies, and realizes a highly efficient and simple preparation process that is suitable for pharmaceutical intermediates and bioconjugates.

CN122444982APending Publication Date: 2026-07-24WUHAN VOCATIONAL COLLEGE OF SOFTWARE & ENG (WUHAN OPEN UNIV)
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Patent Information

Application Number
CN202610663086.9
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-05-14
Publication Date
2026-07-24

AI Technical Summary

Technical Problem

Existing technologies are difficult to use efficiently to prepare pure free amino-polyethylene glycol-propionic acid, as the process is cumbersome and the product form is not easy to control.

Method used

Under neutral conditions, the synergistic effect of cerium chloride heptahydrate and sodium iodide was utilized to deprotect the single molecular weight BocNH-polyethylene glycol-tert-butyl propionate in a one-pot process, thereby simultaneously releasing the amino and carboxyl groups and obtaining the pure free target compound.

Benefits of technology

It simplifies the process flow, improves product purity and stability, is easy to operate, and has a yield of 75%-92%. It is suitable for the preparation of monodisperse polyethylene glycol derivatives with various chain lengths and is applicable to the synthesis of pharmaceutical intermediates and bioconjugation.

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Abstract

The invention provides a synthesis method of free-state single-molecular-weight amino-polyethylene glycol-propionic acid, and relates to the technical field of preparation of amino-polyethylene glycol-propionic acid. The synthesis method of the free-state single-molecular-weight amino-polyethylene glycol-propionic acid comprises the following steps: mixing single-molecular-weight BocNH-polyethylene glycol-tert-butyl propionate with cerium chloride heptahydrate, sodium iodide and an organic solvent under a neutral condition, then carrying out a heat preservation reaction, and after the reaction is completed, carrying out purification and extraction to obtain the free-state single-molecular-weight amino-polyethylene glycol-propionic acid. The free-state single molecular weight amino-polyethylene glycol-propionic acid is obtained. According to the method, one-pot deprotection is directly performed on BocNH-polyethylene glycol-tert-butyl propionate with single molecular weight by utilizing the synergistic effect of cerium chloride heptahydrate and sodium iodide, simultaneous dissociation of amino and carboxyl is realized, a pure free target compound is obtained, the process is simple, the condition is mild, the product form is controllable, and the method is suitable for industrial production. Wide application prospects are shown in the fields of medicine intermediate synthesis and biological coupling.
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